NEW PHOSPHINANE AND AZAPHOSPHINANE DERIVATIVES, THEIR PREPARATION PROCESS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Abstract

Compounds of formula (I) in which: Ak1 represents an alkyl chain, X represents -(CH2)m-, -CH(R)-, -N(R)-,-CH2-N(R)-, –N(R)-CH2- or -CH2-N(R)-CH2-, m and R are as defined in the description, R1 and R2 each represent H when X represents -(CH2)m-, -CH(R)-, -N(R)-, -CH2-N(R)- or –N(R)-CH2-, or indeed together form a bond when X represents -CH2-N(R)-CH2-, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yle, Cy and Ak3 are as defined in the description, R4 and R5, identical or different, each represent H or F, the optical isomers of same, and the pharmaceutically acceptable acid addition salts thereof. The invention also relates to drugs containing same.

Description

NEW DERIVATIVES OF PHOSPHINANES AND AZAPHOSPHINANES, THEIR PREPARATION PROCESS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM The subject of the present invention is novel derivatives of phosphinanes and azaphosphinanes, their method of preparation and the pharmaceutical compositions which contain them. The compounds of the invention are TAFIa (activated thrombin-activatable fibrinolysis inhibitor) inhibitors. TAFI (also called plasma procarboxypeptidase B, procarboxypeptidase R or procarboxypeptidase U) is a 60 kDa plasma glycoprotein produced by the liver that circulates as a zymogen. During coagulation and blood fibrinolysis, thrombin and plasmin cleave the prosegment of TAFI at the Arg92-Ala93 bond to transform it into an active enzyme, TAFIa, whose half-life is 8 to 15 minutes at 37 °C. Prosegment cleavage by thrombin is accelerated by thrombomodulin, a cofactor present in plasma and on the surface of endothelial vascular cells (Bouma BN and Meijers JC, Thrombin-activatable fibrinolysis inhibitor, 2003, Journal of Thrombosis and Haemostasis, 1: 1566-1574). TAFIa negatively regulates fibrinolysis by cleaving the C-terminal lysine residues of fibrin fibers that appear during partial degradation of fibrin by the first traces of plasmin. These C-terminal lysine residues on partially degraded fibrin behave as ligands for circulating plasma plasminogen and tissue plasminogen activator (tPA) generated by endothelial cells during thrombotic ischemia. They thus make it possible to localize the transformation of plasminogen into plasmin by tPA without interference either with the circulating inhibitor of plasmin a2-antiplasmin or with the circulating inhibitor of tissue plasminogen activator (PAI-1). The cleavage of the C-terminal lysine sites by TAFIa therefore decreases the rate of generation of plasmin. Endogenous fibrinolysis is then inhibited and the lysis of fibrinous arterial and venous thrombosis as well as the therapeutic thrombolysis undertaken in patients in the post-thrombotic acute ischemic phase are also reduced. TAFIa inhibitors therefore have the potential to increase endogenous and therapeutic fibrinolysis and to behave as antithrombotic and profibrinolytic agents without major hemorrhagic risk since they interfere neither with platelet activation nor with coagulation during blood hemostasis. The inhibition property of TAFIa therefore makes it possible to envisage the use of the compounds of the invention in the treatment and prevention of thrombotic events in patients at risk. Their use will be interesting in the treatment, prevention and secondary prevention of vascular complications, more particularly cardiovascular, pulmonary and cerebrovascular related to atherothrombotic diseases, atherosclerosis, diabetes, hyperlipidemia, hypertension, chronic venous disorders, metabolic syndrome linked to obesity or cancer. The compounds according to the invention are particularly useful for the treatment, prevention and secondary prevention of myocardial infarction, angina pectoris, cerebrovascular accidents, aortic aneurysms, arteritis of the lower limbs, fibrotic diseases, venous thrombosis and pulmonary embolism. Vascular risk factors and vascular diseases such as hypertension, obesity, diabetes, heart disease, cerebrovascular disease and hyperlipidemia and therefore atherosclerosis play a role in the genesis of dementias such as the disease Alzheimer's and vascular dementia (Qiu C, De Ronchi D. And Fratiglioni L., The epidemiology of the dementias: an update, 2007, Current Opinion in Psychiatry, 20: 380-385). The compounds of the invention will therefore also be useful for the treatment and / or prevention of dementias such as Alzheimer's disease and vascular dementia. TAFIa decreases the endogenous fibrinolytic potential. As TAFIa inhibitors, the compounds of the present invention are therefore useful to accompany acute treatment with injectable fibrinolytics, such as recombinant tPA (for example alteplase, tenecteplase, reteplase, desmoteplase), recombinant uPA or streptokinase, which are used in emergency situations (eg myocardial infarction, stroke). The compounds of the present invention reinforce the activity of these injectable fibrinolytics and therefore lead to their use with less haemorrhagic and neurotoxic risks (reduction of their dose and therefore reduction of their side effects). The present invention relates more especially to the compounds of formula (I): in which Aki represents a C1-C alkyl chain 6 , X represents -(CH 2 ) m -, -CH(R)-, -N(R)-, -CH 2 -N(R)-, -N(R)-CH 2 - or -CH 2 -N(R)-CH 2 -, m represents 0 or an integer from 1 to 4, R represents a hydrogen atom or a group chosen from Ci-C alkyl 6 , -Ak 2 -Ak 2 -Ari-Ar 2 and -Ak 2 -Ari-0-Ar 2 , -Ak 2 -cycloalkyl or -Ak 2 -OH, Ak 2 represents a linear or branched C 1 -C alkyl chain 6 , Ari and Ar 2 , which are identical or different, each represent an aryl or heteroaryl group, Ri and R 2 each represent a hydrogen atom when X represents -(CH 2 ) m -, -CH(R)-, -N(R)-, -CH 2 -N(R)- or -N(R)-CH 2 -, or together form a bond when X represents -CH 2 -N(R)-CH 2 -, R 3 represents NH 2 , Cy-NH 2 , Cy-Ak 3 -NH 2 or piperidin-4-yl, Cy represents a group chosen from cycloalkyl, aryl and heteroaryl, Ak 3 represents a C1-C alkyl chain 3 , R4 and R 5 , which are identical or different, each represent a hydrogen atom or a fluorine atom, their optical isomers, and their addition salts with a pharmaceutically acceptable acid. By aryl group is meant phenyl, naphthyl or biphenyl optionally substituted by one or more groups, identical or different, chosen from halogen, hydroxy, amino, alkyl (Here-C 6 ) linear or branched optionally substituted by one or more halogen atoms, methylsulfonyl, methylthio, carboxy, alkoxy (Ci-C 6 ) linear or branched optionally substituted by one or more halogen atoms, aminoalkyl (Ci-C 6 ) linear or branched, the amino group of the aminoalkyl group being optionally substituted by one or two alkyl groups (Ci-C 6 ) linear or branched. By heteroaryl group is meant an aromatic monocyclic group or an aromatic or partially aromatic bicyclic group, of 5 to 12 members, containing one, two or three heteroatoms chosen from oxygen, nitrogen or sulphur, it being understood that the heteroaryl may optionally be substituted by one or more groups, identical or different, chosen from halogen, hydroxy, amino, oxo, alkyl (Ci-C 6 ) linear or branched optionally substituted by one or more halogen atoms, alkoxy (Ci-Ce) linear or branched optionally substituted by one or more halogen atoms, aminoalkyl (Ci-C 6) linear or branched, the amino group of the aminoalkyl group being optionally substituted by one or two alkyl groups (Ci-C 6 ) linear or branched. Among the heteroaryl groups, mention may be made, without limitation, of the groups pyridyl, thienyl, furyl, imidazolyl, pyrimidinyl, pyrazolyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazinyl, pyridazinyl benzofuryl, benzothienyl, benzimidazolyl, imidazopyridinyl, isoquinolinyl, dihydroquinolinyl furyl, dihydrobenzoxazolyl, dihydroindolyl, dihydroindazolyl, benzodioxolyl. By cycloalkyl group is meant a monocyclic hydrocarbon group, saturated, with 5 to 7 members, it being understood that the cycle can be optionally substituted by one or more groups, identical or different, chosen from halogen, alkyl (Ci-C 6 ) linear or branched. Among the cycloalkyl groups, mention may be made, without limitation, of the cyclopentyl, cyclohexyl and cycloheptyl groups. By optical isomers is meant diastereoisomers and enantiomers. The compounds of formula (I) have at least one asymmetric center: When the configuration of a compound of formula (I) having a single asymmetric center is not specified, the latter is obtained in the form of a mixture of the two enantiomers. When the configuration of a compound of formula (I) having two asymmetric centers is not specified, the latter is obtained in the form of a mixture of diastereoisomers. Among the pharmaceutically acceptable acids, mention may be made, without limitation, of hydrochloric, hydrobromic, sulfuric, phosphoric, acetic, trifluoroacetic, lactic, pyruvic, malonic, succinic, glutaric, fumaric, tartaric, maleic, citric, ascorbic, oxalic, methanesulfonic acids. , benzenesulfonic, β-toluenesulfonic, camphoric. One aspect of the present invention relates to the compounds of formula (I) for which Aki represents -(CH 2 ) 4 -. Another aspect of the present invention relates to the compounds of formula (I) for which X represents -N(R)-. Another aspect of the present invention relates to the compounds of formula (I) for which X represents -N(R)-, -CH 2 -N(R)-, -N(R)-CH 2 - or -CH 2 -N(R)-CH 2 -, and R represents a group chosen from -Ak 2 -Ari, -Ak 2 -Ari-Ar 2 and -Ak 2 -Ari-0-Ar 2 . Another aspect of the present invention relates to the compounds of formula (I) for which X represents -N(R)-, -CH 2 -N(R)-, -N(R)-CH 2 - or -CH 2 -N(R)-CH 2 -, R represents a group chosen from -Ak 2 -Ari, -Ak 2 -Ari-Ar 2 and -Ak 2 -Ari-0-Ar 2 , and Ak 2 represents -CH 2 -. Another aspect of the present invention relates to the compounds of formula (I) for which Ri and R 2 each represent a hydrogen atom. Another aspect of the present invention relates to the compounds of formula (I) for which R 3 represents NH 2 . Another aspect of the present invention relates to the compounds of formula (I) for which R4 and R5 each represent a hydrogen atom. Another aspect of the present invention relates to the compounds of formula (I) for which Ri, R 2 , R4 and R 5 each represent a hydrogen atom, R3 represents NH 2 , X represents -N(R)-, -CH 2 -N(R)-, -N(R)-CH 2 - or -CH 2 -N(R)-CH 2 -, and R represents a group chosen from -Ak 2 -Ar l s -Ak 2 -Ari-Ar 2 and -Ak 2 -Ari-0-Ar 2 . Another aspect of the present invention relates to the compounds of formula (Ia), particular case of the compounds of formula (I): in which Ra represents a group chosen from -CH 2 -Ari and -CH 2 -Ari-Ar 2 , where Ari and Ar 2 are as defined in formula (I). A subject of the present invention is also the process for preparing the compounds of formula (I) from the compound of formula (II): where X, Ri, R 2 , R4 and R 5 are as defined in formula (I), Y represents an alkoxy group C 1 -C4 linear or branched or dialkylamino in which the alkyl groups are Ci-C 4 , linear or ramified, reacted with CO(OG) 2 , where G represents a protective group for the acid function such as alkyl or benzyl, preferably tert-butyl or benzyl, in the presence of a base, to lead to the compound of formula (III): where X, Y, Ri, R 2 and G are as defined previously, which is reacted, in the presence of a base, with the compound Br-Aki-R' 3 , where Aki is as defined in formula (I), and R' 3 represents N(Boc) 2 , Cy-N(Boc) 2 , Cy-Ak 3 -N(Bock) 2 or N-Boc-piperidin-4-yl, to lead to the compound of formula (IV): where X, Y, Ri, R 2 , G, Aki and R' 3 are as previously defined, the amino, carboxy and phosphine functions of which are deprotected, to yield the compound of formula (I) or one of its addition salts with a pharmaceutically acceptable acid. The compound of formula (IV) comprises at least two asymmetric centers: The diasteroisomers of the compound of formula (IV) can be separated using a chiral column, making it possible to obtain optically pure compounds of formula (I) by the process described above. The nomenclature (3aR*, 4S*, 6aS*), used for octahydrophospholo[3,4-c]pyrrole derivatives, indicates a relative configuration. It means that the compound is in the form of a mixture of compounds of absolute configurations (3aR, 4S, 6aS) and (3aS, 4R, 6aR). The present invention also relates to the process for preparing the compounds of formula (Ia), particular case of the compounds of formula (I), from the compound of formula (IVa), special case of compounds of formula (IV): where Y and G are as defined in formula (II), and Ga represents a protective group for the amino function such as Boc, which is debenzylated, to yield the compound of formula (V): where Y, G and Ga are as defined above, which is subjected to a reductive amination reaction with the aldehyde of formula R é -CHO, where Re represents -Ari or -Ari-Ar 2 , where Ari and Ar 2 are as defined in formula (I), to lead to the compound of formula (VI): where Y, G, Ga and Ra are as previously defined, the amino, carboxy and phosphine functions of which are deprotected, to yield the compound of formula (Ia) or one of its addition salts with a pharmaceutically acceptable acid. The compound of formula (IVa) comprises two asymmetric centers: The diasteroisomers of the compound of formula (IVa) can be easily separated using a chiral column, making it possible to obtain optically pure compounds of formula (Ia) by the process described above. The compounds of the invention are TAFIa inhibitors. As such, they are useful in the prevention or treatment of thrombotic events in patients at risk. Their use will be interesting in the treatment and prevention of vascular complications, more particularly cardiovascular, pulmonary and cerebrovascular related to atherothrombotic diseases, atherosclerosis, diabetes, hyperlipidemia, hypertension, chronic venous diseases, metabolic syndrome linked to obesity or cancer. The compounds according to the invention are particularly useful for the treatment, prevention and secondary prevention of myocardial infarction, angina pectoris, cerebrovascular accidents whatever their origin (in particular atherothrombotic, cardioembolic or caused by atrial fibrillation), aortic aneurysms or arteritis of the lower limbs, venous thrombosis (particularly in catheterized cancer patients) and pulmonary embolism. Vascular risk factors and vascular diseases such as hypertension, obesity, diabetes, heart disease, cerebrovascular disease and hyperlipidemia and therefore atherosclerosis play a role in the genesis of dementias such as the disease Alzheimer's and vascular dementia (Qiu C, De Ronchi D. And Fratiglioni L., The epidemiology of the dementias: an update, 2007, Current Opinion in Psychiatry, 20: 380-385). The compounds of the invention will therefore also be useful for the treatment and / or prevention of dementias such as Alzheimer's disease and vascular dementia. TAFIa decreases the endogenous fibrinolytic potential. As TAFIa inhibitors, the compounds of the present invention are therefore useful to accompany acute treatment with injectable fibrinolytics, such as recombinant tPA (for example alteplase, tenecteplase, reteplase, desmoteplase), recombinant uPA or streptokinase, which are used in emergency situations (eg myocardial infarction, stroke). The compounds of the present invention reinforce the activity of these injectable fibrinolytics and therefore lead to their use with less haemorrhagic and neurotoxic risks (reduction of their dose and therefore reduction of their side effects). A subject of the present invention is also the pharmaceutical compositions containing a compound of formula (I), in combination with one or more excipients or inert, non-toxic, pharmaceutically acceptable vehicles. The useful dosage varies according to the age and weight of the patient, the route of administration, the nature and severity of the condition, and the taking of any associated treatments and ranges from 0.5 mg to 1000 mg in one or more doses per day. Among the pharmaceutical compositions according to the invention, mention will be made more particularly of those which are suitable for oral, parenteral (intravenous, intramuscular or subcutaneous), per or transcutaneous, nasal, rectal, perlingual, ocular or respiratory administration, and in particular plain or sugar-coated tablets, sublingual tablets, capsules, capsules, suppositories, creams, ointments, dermal gels, injectable or drinkable preparations, aerosols, eye or nasal drops. According to one aspect of the present invention, the pharmaceutical composition is an injectable preparation for intravenous administration. According to another aspect of the present invention, the pharmaceutical composition is a tablet for oral administration. Besides the compound of formula (I), the tablets according to the invention contain one or more excipients or vehicles such as diluents, lubricants, binders, disintegrating agents, absorbents, colorants, sweeteners. By way of example of excipients or vehicles, mention may be made of: ♦ for diluents: lactose, dextrose, sucrose, mannitol, sorbitol, cellulose, glycerine, ♦ for lubricants: silica, talc, stearic acid and its magnesium and calcium salts, polyethylene glycol, ♦ for binders: magnesium aluminum silicate, starch, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose and polyvinylpyrrolidone, ♦ for disintegrants: agar, alginic acid and its sodium salt, effervescent mixtures. The percentage of active principle of formula (I) in the tablet is preferably between 5% and 50% by weight. According to one aspect of the present invention, the compound of formula (I) according to the present invention is administered in combination with a fibrinolytic, more particularly an injectable fibrinolytic such as recombinant tPA (for example alteplase, tenecteplase, reteplase or desmoteplase), the uPA or streptokinase, or with an anticoagulant such as, for example, warfarin, dabigatran etexilate, rivaroxaban. The administration in association can be in the form of a simultaneous or successive co-administration of two separate pharmaceutical compositions each containing one of the active principles (free association), or in the form of the administration of a fixed association of the two active principles within the same pharmaceutical composition. According to one aspect of the present invention, the compound of formula (I) is administered in the form of an injectable preparation, in free association with an injectable preparation of alteplase. According to another aspect of the present invention, the compound of formula (I) is administered in the form of an injectable preparation, in free association with an injectable preparation of tenecteplase. The following examples illustrate the present invention. The structures of the compounds described in the examples were determined according to the usual spectrophotometric techniques (infrared, nuclear magnetic resonance, mass spectrometry). ABBREVIATIONS AcOEt: ethyl acetate AIBN: azobisisobutyronitrile DCM: dichloromethane DEA: diethylamine DIBA1H: diisobutylaluminum hydride DMAP: dimethylaminopyridine DMF: dimethylformamide DMSO or dmso: dimethyl sulfoxide OD: optical density EDTA: ethylenediaminetetraacetic acid eq: molar equivalent HMPA: hexamethylphosphoramide HPLC: high performance liquid chromatography IR: infrared LDA: lithium diisopropylamide LiHMDS: lithium hexamethyldisilazane or lithium bis(trimethylsilyl)amide MTBE: methyl tert-butyl ether PR: optical rotation NMR: Nuclear Magnetic Resonance TAFIa: activated thrombin-activatable fibrinolysis inhibitor TEA: triethylamine TFA: trifluoroacetic acid THF: tetrahydrofuran TMS: trimethylsilyl tPA: tissue plasminogen activator uPa: urokinase-type plasminogen activator (urokinase plasminogen activator) or urokinase Xantphos: 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene Side Chain Synthesis Procedure - Procedures I, J, K (Intermediate 204-212) Intermediate 204 Procedure I: To a solution of di-tert-butyl iminodicarboxylate (20 g, 92 mmol) in IL of DMF under an Argon atmosphere and at room temperature is added portions of cesium carbonate (60 g, 184 mmol, 2 eq ). Vigorous stirring is maintained for 1 hour before adding 1,4-dibromobutane (99.2 g, 459 mmol, 5 eq). After 24 hours at room temperature, the reaction mixture is filtered through Celite and concentrated under reduced pressure. The residue obtained is purified by flash chromatography on silica gel using a heptane / AcOEt (100% to 90:10) gradient as eluent. Intermediate 204 (26.1 g, 74.1 mmol) is obtained in the form of a colorless oil with a yield of 81%. Intermediate 204 1H NMR: (CDCls, 400 MHz) δ 3.60 (t, 2 H), 3.42 (t, 2 H), 1.87 (quint., 2 H), 1.73 (quint., 2 H), 1.51 (s, 18 H ). IRi 1790-1744-1693 cm "1 (C=0), 1125cm "1 (CO). Intermediate 205 Intermediate 205 is obtained from 1,3-dibromopropane according to procedure I previously described. Product isolated in the form of a colorless oil (24.7 g, 73.0 mmol) with a yield of 79%. 1H NMR: (CDCl3, 400 MHz) δ 3.6 (m, 2H), 3.5 (t, 2H), 2.05 (quint., 2H), 1.51 (s, 18H). IR: 1791-1744-1693cm "1 (C=0), 1125cm "1 (CO). Intermediate 206 Intermediate 206 is obtained from 1,5-dibromopentane according to procedure I previously described. Product obtained in the form of a colorless oil (27.9 g, 76.2 mmol) with a yield of 83%. 1H NMR: (CDCI3, 400 MHz) δ 3.60 (t, 2 H), 3.40 (t, 2 H), 1.90 (m, 2 H), 1.60 (m, 2 H), 1.45 (m, 2H), 1.50 (s, 18H) ppm. IR: 1740, 1693 (C=0), 1787cm "1 (C=0 low). Intermediate 207 Intermediate 207 is obtained from 1,6-dibromohexane according to procedure I previously described. 1H NMR: (CDCk 400 MHz) δ 3.58 (t, 2H), 3.40 (t, 2H), 1.89 (m, 2H), 1.65-1.25 (m, 6H), 1.45 (m, 6H), 1.51 (s, 18H) ppm. Procedure J Intermediate 208 To a suspension of 60% NaH (0.682 g, 17 mmol, 1.5 eq) in a mixture of THF (25 mL) and DMF (3 mL) under argon and at room temperature, are added portion by portion of tert-butyliminodicarboxylate (2.47 g, 11.37 mmol, 1 eq). The reaction medium is stirred at ambient temperature for 15 minutes and then warmed to 45° C. for 45 minutes. This suspension is then added to a solution of 1,3-dibromomethylbenzene (3 g, 11.37 mmol, 1 eq) in THF (100 mL). Stirring continues at room temperature for 16 h. The mixture is hydrolyzed dropwise with a solution of NH 4 10% C1 (100mL). The organic phase is extracted with AcOEt (2 x 50 mL), washed with a saturated NaCl solution (50 mL) and dried over MgS0 4 . The solvent is evaporated off under reduced pressure and the crude is purified by flash chromatography on silica gel using a gradient as eluent Heptane / DCM (50:50 to 100%). Intermediate 208 (2.07 g, 5.17 mmol) is obtained in the form of a colorless oil with a yield of 45%. 1H NMR: (DMSO-dg, 400 MHz) δ 7.33 (d, 2 H), 7.3 (si, 1 H), δ 3.15 (t, 1 H), 4.70 / 4.68 (2s, 4 H), 1.40 (s , 6 p.m.). IR; 1790-1747-1699cm "1 (C=0), 1224-1143-1110cm "1 (C-O-C), 854-781-699 cm "1 (Tank). MS^ m / z 422 [M+Na]. Intermediate 209 Intermediate 209 is obtained from 1,4-dibromomethylbenzene according to procedure J previously described. Obtaining a white solid (2.02 g, 5.05 mmol) with a yield of 44%>. 1H NMR: (DMSO-dg, 400 MHz) δ 7.40 (d, 2H), 7.20 (d, 2H), 4.69 (2s, 4H), 1.39 (s, 18H). IR_: 1767-1693cm "1 (C=0). MS: m / z 343 [M-C 4 H 8 ]. K-procedure Intermediate 210 Diisopropylethylamine (59.34 g, 462 mmol, 2 eq). A solution of (Boc) 2 0 (125.5 g, 575 mmol, 2.5 eq) is then added dropwise followed by N,N-dimethylaminopyridine (28.1 g, 230 mmol, 1 eq). The reaction mixture is stirred for 15 h at room temperature. The aqueous phase is extracted with AcOEt (2×400 mL). The organic phases are combined, washed with a solution of NH 4 10% CI (400 mL), with a saturated NaCl solution (400 mL), with a 10% NaHCC"3 solution (400 mL) and finally with a saturated NaCl solution (400 mL). The organic phase is dried over MgSC 4 and the solvent is evaporated off under reduced pressure. The residue obtained is purified by flash chromatography on silica gel using a heptane / AcOEt (90:10 to 75:25) gradient as eluent. Intermediate 210 ( 32.78 g, 106.3 mmol) is obtained in the form of a colorless oil with a yield of 46%. 1H NMR: (400 MHz, CDC13) δ ppm 8.3 (s, 1H), 7.75 (dd, 1H), 7.1 (d, 1H), 2.3 (s, 3H), 1.45 (s, 18H) IR: 1742-1707 cm' (C=0). Intermediate 211 To a solution of intermediate 210 (3.08 g, 10 mmol) and N-bromosuccinimide (1.87 g, 10.5 mmol, 1.05 eq) in CCI 4 (50 mL) is added with AIBN (0.164 g, 1 mmol). The reaction medium is refluxed for 20 h. Once at room temperature, the insolubles are filtered off and the filtrate is concentrated under reduced pressure. The residue is purified by flash chromatography on silica gel using a DCM / AcOEt gradient (from 99:1 to 95:5) as eluent. Intermediate 211 (2.15 g, 5.56 mmol) is obtained in the form of a white solid with a yield of 56%. 1H NMR: (400 MHz, CDC13) δ ppm 8.55 (d, 1H), 7.75 (dd, 1H), 7.3 (d, 1H), 4.45 (s, 2H), 1.45 (s, 18H) IR: 1753-1743-1710 cm' (C=0). Intermediate 212 Intermediate 212 is obtained from 2-amino-4-methylpyridine according to procedure K previously described. 1H NMR: (400 MHz, CDC13) δ ppm 8.48 (d, 1H), 7.3 (d, 1H), 7.22 (d, 1H), 4.4 (s, 2H), 1.45 (s, 18H) IR: 1788-1755-1724cm _1 (C=0). Procedure A - synthesis of examples 1 to 19. Stadium Al m = 0 to 4 To a solution of hypophosphorous acid (7.42 g, 112 mmol, 1.0 eq) in acetonitrile (160 mL) under argon and at room temperature is added tetraethylorthosilicate (25 mL, 112 mmol, 1.0 eq). The reaction mixture is heated at reflux for 2h30 and then cooled to room temperature. Bromoalkene CH 2 =CH-(CH 2 ) m +2-Br (0.5 eq), Pd 2 dba 3 (0.769 g, 0.84 mmol) and Xantphos (0.356 g, 0.62 mmol) are then added and the reaction mixture is heated at reflux for 18 h. The solution is then filtered through filter paper at ambient temperature, and concentrated under reduced pressure. The crude is purified by flash chromatography on a silica column using a heptane / AcOEt gradient as eluent. The compound of stage Al is obtained in the form of an oil. Stage A2 m = 0 to 4 To a solution degassed with argon for 30 min of the compound of stage Al (233 mmol, 1 eq) in THF (870 mL) at -78° C. is added dropwise a solution of LiHMDS at 1.06M / THF (220 mL, 1.0 eq). After addition, the reaction mixture is stirred at room temperature for 2h30. The reaction is then quenched at 0° C. by adding a saturated aqueous solution of NaCl (870 mL). After extraction with ethyl acetate (3 x 800 mL), the organic phases are combined, washed with a saturated solution of NaCl, dried over MgS0 4 before being concentrated under reduced pressure. The crude is then purified by flash chromatography on a silica column using a 95:5 DCM / EtOH mixture as eluent. The compound of stage A2 is obtained in the form of an oil. Stage A3 m = 0 to 4 To a solution of the compound of stage A2 (8.5 mmol, 1 eq) in THF (20 mL) at −70° C. and under a flow of argon, is added LDA (6.4 mL, 12.8 mmol, 1.5 eq). Stirring is maintained for 20 min. A solution of dibenzylcarbonate (2.88 g, 11.9 mmol, 1.4 eq) in THF (11 mL) is then added dropwise. The mixture is stirred for 45 min, then a second addition of LDA (6.4 mL, 12.8 mmol, 1.5 eq) is carried out. The solution is stirred for 2 hours at -70°C. A solution of NH 4 C1 at 10% (60 mL) is then added dropwise while maintaining the temperature of the reaction mixture at -70°C. AcOEt (20 mL) is then added and the reaction medium is gradually brought up to ambient temperature. The reaction mixture is then extracted with AcOEt (2 x 80 mL). The organic phases are combined and dried over MgS0 4 , filtered and concentrated under reduced pressure. The crude is purified by flash chromatography on a silica column using a DCM / EtOH gradient as eluent. The compound of stage A3 is obtained in the form of an oil. Stage A4 m, Aki as defined in formula (I) A suspension of 60% NaH (0.448 g, 11.14 mmol) in 5 mL of DMSO at 10°C and under Argon is successively added to a solution of intermediate 204 to 212 (7.65 mmol, 1.1 eq.) in 8 ml of DMSO then, drop by drop, a solution of the compound of stage A3 (6.96 mmol, 1 eq) in 5 ml of DMSO. At the end of the addition, the reaction mixture is brought back to room temperature and stirred for 3 hours. The treatment is carried out at 0°C by adding NH 4 C1 10% (100 mL) then AcOEt (100 mL). After decantation, the aqueous phase is re-extracted with AcOEt (2×80 mL). The organic phases are combined, washed with a saturated NaCl solution (2 x 80 mL), dried over MgS0 4 , filtered and concentrated under reduced pressure. The crude is purified by flash chromatography on a silica column using a DCM / EtOH gradient as eluent. The compound of stage A4, a mixture of diastereoisomers, is obtained in the form of a colorless oil. Stage A5 m, Aki as defined in formula (I) Bromotrimethylsilane (0.721 mL, 5.47 mmol, 8 eq) is added dropwise to a solution of the compound of stage A4 (0.683 mmol, 1.0 eq) in DCM (30 mL) at 0° C. and under Argon. The mixture is stirred for 20 h at room temperature. Evaporation under reduced pressure is carried out then the mixture is evaporated to dryness using a vane pump for 30 min. The mixture is taken up in MeOH (30 mL), stirred for 30 min, then evaporated under reduced pressure and to dryness using a vane pump for 30 min. The mixture is again taken up in MeOH, stirred, and evaporated. This operation is performed a third time. The compound of stage A5 is obtained in the form of the hydrobromide salt and is used directly in the following hydrogenation reaction. Stage A6 - Examples 1 to 19 To a solution of the compound of stage A5 in MeOH (15 mL), is added Pd / C (10 mol%) at 10%. The mixture is stirred for 18 h under an H atmosphere 2 at room temperature. The catalyst is filtered through a Whatman sinter. The filtrate is evaporated to dryness. 12 eq of TFA are added to the crude. The product is purified by flash chromatography on a reverse phase RP18 column using an H gradient 2 O / MeCN / TFA as eluent. After freeze-drying, the expected product (examples 1 to 19), TFA salt, is obtained in the form of a hygroscopic white solid. EXAMPLE 1: 2-(3-Aminopropyl)-l-hydroxy-l-oxo-l-phospholane-2-carboxylic acid, trifluroacetate Example 1 is obtained from intermediate 205 according to procedure A previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 12-11 (si, 1H), 8.3-7.3 (si, 3H), 2.8 (q, 2H), 2.25 (m, 1H), 1.9 ( m, 1H), 1.8-1.4 (m, 8H) ESI / FIA / HR and MS / MS: ESI + / -: infusion: [M+H]+ = 222.1 Elemental Analysis: C=35.39(35.83);H=5.44(5.11);N=4.60(4.18) EXAMPLE 2: 2-(4-Aminobutyl)-l-hydroxy-l-oxo-l-phospholane-2-carboxylic acid, trifluroacetate Example 2 is obtained from intermediate 204 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 12.5 (si, 1H), 7.75 (si, 3H), 2.8 (q, 2H), 2.21-1.6 (m, 2H), 1.9-1.35 ( m, 2H), 1.8-1.5 (m, 6H), 1.6-1.2 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 236.1041 (236.1051) Elemental Analysis: C=38.94(37.83);H=5.81(5.48);N=4.50(4.01) EXAMPLE 3: 2-[(6-aminopyridin-3-yl)methyl]-l-hydroxy-l-oxo-l-phospholane-2-carboxylic acid, trifluroacetate Example 3 is obtained from intermediate 211 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 13 (si, 2 H), 7.9 (si, 3 H), 7.7 (m, 2 H), 6.85 (d, 1 H), 3.2 (m, 1 H), 2.7 (m, 1H), 2.05 (m, 1H), 1.85-1.5 (m, 5H) ESI / FIA / HR and MS / MS: [M+H]+ = 271.0842 (271.0847) Anal y se Elementary: C=41.20(40.64);H=4.52(4.20);N=8.06(7.29) EXAMPLE 4: 2-(5-Aminopentyl)-1-hydroxy-1-oxo-1-phospho]ane-2-carboxylic acid, trifluroacetate Example 4 is obtained from intermediate 206 according to procedure A previously described. NMR Ή: (300 MHz, dmso-d6) δ ppm 12.5 (si, 1H), 2.78 (m, 2H), 1.8 to 1.4 (m, 4H), 7.68 (si, 3H), 2.22 / 1.65 (m, 2H), 1.98 / 1.3 (m, 2H), 1.52 (t, 2H), 1.4 to 1 (m, 4H) ESI / FIA / HR and MS / MS: [M+H]+ = 250.1209 (250.1208) Elemental Analysis: C=39.69(39.68);H=5.91(5.83);N=4.37(3.86) EXAMPLE 5: 2-(3-Aminopropyl)-1-hydroxy-1-oxo-1-phosphinane-2-carboxylic acid , trifluroacetate Example 5 is obtained from intermediate 205 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 13.0 (si, 1H), 7.73 (si, 3H), 2.77 (m, 2H), 1.93-1.66- 1.44 (3*(m, 2+ 10H) ESI / FIA / HR and MS / MS: [M+H]+ = 236.1051 (236.1051) Elemental Analysis: C=38.07(37.83);H=5.85(5.48);N=4.1 1(4.01) EXAMPLE 6: 2-(5-Aminopentyl)-1-hydroxy-1-oxo-1-phosphinane-2-carboxylic acid, trifluroacetate Example 6 is obtained from intermediate 206 according to procedure A previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.65 (si, 3H), 2.75 (m, 2H), 1.9 (m, 2H), 1.0-1.85 (m, 14H) E SI / FI A / HR and M S / M S: ESI + / -: infusion: [M+H]+ = 264.1 Elemental Analysis: C=40.84(41.39);H=5.66(6.14);N=3.76(3.71) EXAMPLE 7: 2-(4-Aminobutyl)-1-hydroxy-1-oxo-1-phosphinane-2-carboxylic acid, trifluroacetate Example 7 is obtained from intermediate 204 according to procedure A previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.68 (si, 3 H), 2.78 (m, 2 H), 2.02 to 1.16 (m, 14 H) ESI / FI A / HR and M S / M S: ESI + / -: infusion: [M+H]+ = 250.1 Elemental Analysis: C=39.61(39.68);H=5.71(5.83);N=3.86(3.86) EXAMPLE 8: 2-(4-Aminobutyl)-1-hydroxy-1-oxo-1-phosphepane-2-carboxylic acid , trifluroacetate Example 8 is obtained from intermediate 204 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 13 to 11.5 (si, 1 H), 7.75 (si, 3 H), 2.8 (m, 2 H), 2.1 to 1.85 (m, 2 H), 1.85 at 1.2 (m, 2 p.m.) ESI / FI A / HR and M S / M S: ESI + / -: infusion: [M+H]+ = 264.1 EXAMPLE 9: 2-[[4-(aminomethyl)phenyl]methyl]-l-hydroxy-l-oxo-l-phospholane-2-carboxylic acid, trifluroacetate Example 9 is obtained from intermediate 209 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 13 to 12 (si, 1 H), 7.39 (d, 2 H), 2.1 to 1.5 (m, 6 H), 7.22 (d, 2 H), 8.3 (si, 3H), 3.98 (m, 2H), 3.39 / 2.75 (2dd, 2H) ESI / FI A / HR and M S / M S: [M+H]+ = 284.1048 (284.1051) Elemental Analysis: C=48.29(48.84);H=5.45(5.99);N=4.64(4.38) EXAMPLE 10: 2-(5-aminopentyl)-1-hydroxy-1-oxo-1-phosphepane-2-carboxylic acid , trifluroacetate Example 10 is obtained from intermediate 206 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 12 (si, 1H), 7.68 (si, 3H), 2.76 (m, 2H), 2.12 to 1.9 (m, 2H), 1.87 to 1.11 (m, 16H) E SI / FI A / HR and M S / M S: [M+H]+ = 278.1518 (278.1521) Elemental Analysis: C=41.99(42.97);H=6.38(6.44);N=3.53(3.58) EXAMPLE 11: 1-Hydroxy-1-oxo-2-(2-piperidin-4-ylethyl)-1-phosphinane-2-carboxylic acid, trifluroacetate Example 11 is obtained from N-Boc-4-bromoethylpiperidine according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 12 (si, 1 H), 8.49-8.2 (2*(m, 2 H), 3.24 (dl, 2 H), 2.82 (m, 2 H), 1.94-1.65-1.45-1.2 (4*(m, 12H), 1.79 (tl, 2H), 1.39 (m, 1H), 1.2 (m, 2H) ESI / FI A / HR and M S / M S: [M+H]+ = 290.1526 (290.1521) Elemental Analysis: C=44.65(44.67);H=5.93(6.25);N=3.41(3.47) EXAMPLE 12: Acid 2-[[3-(aminomethyl)phenyl]methyl]-l-hydroxy-l-oxo-l - phosphinane-2-carboxylic acid, trifluroacetate Example 12 is obtained from intermediate 208 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.19 (si, 3H), 7.3 (m, 2H), 7.22 (s, 1H), 7.14 (d, 1H), 3.99 (m, 2 H), 3.32 / 2.97 (2dd, 2H), 1.9 to 1.4 (m, 8H) ESI / FI A / HR and M S / M S: [M+H]+ = 298.12 (298.120821) Elemental Analysis: C=47.00(46.72);H=4.82(5.15);N=3.39(3.41) EXAMPLE 13: 2-(6-Aminohexyl)-1-hydroxy-1-oxo-1-phosphinane-2-carboxylic acid, trifluoroacetate Example 13 is obtained from intermediate 207 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.65 (si, 3 H), 2.77 (m, 2 H), 1.93 (m, 2 H), 1.8 to 1.14 (m, 16 H) E SI / FI A / HR and M S / M S: [M+H]+ = 278.1522 (278.15212) Elemental Analysis: C=42.69(42.97);H=6.26(6.44);N=3.79(3.58) EXAMPLE 14: 2-(4-Aminobutyl)-1-hydroxy-1-oxo-1-phosphocane-2-carboxylic acid, trifluoroacetate Example 14 is obtained from intermediate 204 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.72 (si, 3 H), 2.8 (m, 2 H), 2.11 to 1.32 (m, 18 H) ESI / FI A / HR and M S / M S: [ M+H]+ = 278.1522 (278.1521) Elemental Analysis: C=43.34(42.97);H=6.35(6.44);N=2.91(3.58) EXAMPLE 15: Acid 2-[(2-aminopyridin-4-yl)methyl]-l-hydroxy-l-oxo- l-phosphinane- 2-carboxylic, trifluoroacetate Example 15 is obtained from intermediate 212 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 13.5 to 12 (si, 1H), 7.8 (d, 1H), 7.87 (si, 3H), 6.75 (s, 1H), 6.6 (d , 1 H), 3.25 / 3 (m, 2 H), 2 to 1.35 (m, 8 H) ESI / FI A / HR and M S / M S: [M+H]+ = 285.1012 (285.1004) EXAMPLE 16: 2-[2-rans-4-aminocyclohexyl)ethyl]-1-hydroxy-1-oxo-1-phosphinane-2-carboxylic acid, trifluoroacetate Example 16 is obtained from tert-butyl [trans-4-(2-bromoethyl)cyclohexyl]carbamate, according to procedure A previously described. 1H NMR: (300 / 400 / 500 MHz, dmso-d6) δ ppm 7.9 (si, 3H), 2.9 (m, 1H), 2.01 (m, 2H), 1.91-1.74 (2m, 4H), 1.64 (m, 2H), 1.53 (m, 2H), 1.39 (m, 2H), 1.29-0.95 (m, 4H), 1.11 (m, 4H), 1.09 (m, 1H) NMR 13 C: (300 / 400 / 500 MHz, dmso-d6) δ ppm 49.8, 36.8, 31.6, 30.8, 30.5, 30.5, 30.5, 23.6, 22.9 ESI / FIA / HR and MS / MS: [M+H]+ = 304.1648 (304.1677) EXAMPLE 17: 2-[2-(cis-4-aminocyclohexyl)ethyl]-1-hydroxy-1-oxo-1-phosphinane-2-carboxylic acid, trifluoroacetate Example 17 is obtained from tert-butyl [cis-4-(2-bromoethyl)cyclohexyl]carbamate, according to procedure A previously described. 1H NMR: (400 / 500 MHz, dmso-d6) δ ppm 7.9 (si, 3H), 3.15 (m, 1H), 1.96-1.62 (2m, 2H), 1.94-1.73 (2m, 2H), 1.71-1.65 (2m, 2H), 1.68-1.65 (2m, 2H), 1.56-1.39 (m, 4H), 1.49-1.36 (2m, 2H), 1.38 (m, 1H), 1.23- 1.16 (2m, 2H) NMR 13 C: (400 / 500 MHz MHz, dmso-d6) δ ppm 173.3, 51, 47.9, 34, 31, 28.7, 27.9, 26.5, 26.5, 23.4, 21.6 NMR 13 C: (400 / 500 MHz, dmso-d6) δ ppm 173.3, 51, 47.9, 34, 31, 28.7, 27.9, 26.5, 26.5, 23.4, 21.6 ESI / FIA / HR and MS / MS: [M+H]+ = 304.1671 (304.1677) Elemental Analysis: C=45.47(46.05);H=6.68(6.52);N=3.58(3.36) EXAMPLE 18: 2-(5-Aminopentyl)-1-hydroxy-1-oxo-1-phosphocane-2-carboxylic acid, trifluoroacetate Example 18 is obtained from intermediate 206 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 12.0-11.0 (si, 1H), 7.7 (m, 3H), 2.8 (m, 2H), 2.05 (m, 2H), 1.9-1.3 ( m, 18H) ESI / FIA / HR and MS / MS: [M+H]+ = 292.1656 (292.1677) Elemental Analysis: C=44.17(44.45);H=6.69(6.71);N=3.42(3.46) EXAMPLE 19: 2-(5-Aminopentyl)-1-hydroxy-1-oxo-1-phosphonane-2-carboxylic acid, trifluoroacetate Example 19 is obtained from intermediate 206 according to procedure A previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 12.4-11 (si, 1H), 7.7 (si, 3H), 2.75 (t, 2H), 2.3 (m, 1 H), 2.05 (m, 1H), 1.9-1.2 (m, 20H) ESI / FIA / HR and MS / MS: [M+H]+ = 306.1834 (306.1834) Elemental Analysis: C=45.54(45.82);H=6.98(6.97);N=3.26(3.34) Procedure B - Synthesis of phosphinanes Stage Bl (Intermediate 6) To a solution of phenylacetaldehyde (28.74 g, 239 mmol) in DCM (380 mL) and at room temperature is added portionwise ethyl (triphenylphosphorylidene)acetate (100 g, 287 mmol, 1.2 eq). The reaction medium is stirred for 20 h at room temperature and then the mixture is concentrated under vacuum. The residue is taken up in heptane (400 mL), stirred for 1 hour then the insoluble matter is filtered off. The heptane is evaporated under vacuum and the residue obtained is purified by flash chromatography on silica gel using a Heptane / DCM (60:40) mixture as eluent. Intermediate 6 (27.25 g, 143 mmol) is obtained in the form of a colorless oil with a yield of 60%. 1H NMR: (400 MHz, CDC13) δ ppm 7.3 (t, 2 H), 7.25 (t, 1 H), 7.2 (d, 2 H), 7.1 (dt, 1 H), 5.8 (d, 1 H) , 4.2 (quad, 2H), 3.5 (d, 2H), 1.3 (t, 3H) IR (cm 1 ): 1716, 1653 Stage B2 (Intermediate 7) To a solution of intermediate 6 (28.35 g, 149 mmol) in DCM (375 mL) at ambient temperature and under an argon atmosphere is added a solution of 1M DIBA1H in THF (355 mL, 355 mmol). After 45 minutes at 0° C., the reaction medium is stirred for 16 h at room temperature. The reaction medium is then cooled to 0° C. and treated with 3N HCl (300 mL). The mixture is extracted with DCM (350 mL), the organic phase is washed with H 2 0 (2 x 100 mL), dried over Na 2 S0 4 then evaporated under vacuum. The residue obtained is purified by flash chromatography on silica gel using a mixture of Heptane / AcOEt (75:25) as eluent. Intermediate 7 (16.05 g, 108 mmol) is obtained in the form of a colorless oil with a yield of 72%. 1H NMR: (400 MHz, CDC13) δ ppm 7.1-7.4 (m, 5H), 5.65-5.9 (2m, 2H), 4.1 (d, 2H), 3.35 (d, 2H), 1.5 (m , 1H) IR (cm 1 ): 3600-3200, 1716, 1650 Stage B3 (Intermediate 8) The mixture of intermediate 7 (3.7 g, 25 mmol), with triethylorthoacetate (16.2 g, 100 mmol, 4 eq) and propionic acid (5 drops) is stirred for 1 hour 20 minutes in a microwave (250 W) at 140° vs. The mixture is resumed with And 2 0 (300mL) and H 2 0 (100mL). The organic phase is then washed with H 2 0 (100 mL), dried over MgSC 4 then concentrated in vacuo. The residue obtained is purified by flash chromatography on silica gel using a mixture of heptane / AcOEt (80:20) as eluent. Intermediate 8 (4.53 g, 20.7 mmol) is obtained in the form of an oil with a yield of 83%. 1H NMR: (400 MHz, CDC13) δ ppm 7.15-7.3 (m, 5 H), 5.7 (m, 1 H), 5 (m, 2 H), 4.1 (q, 2 H), 2.85 (m, 1 H), 2.7 (m, 2H), 2.25-2.4 (m, 2H), 1.25 (t, 3H) IR (cm _1 ): 1732, 699-747 Stage B4 (Intermediate 9) To a solution of intermediate 8 (17.58 g, 80.5 mmol) in THF (275 mL) at 0°C and under Argon, is added in portions L1AIH 4 (6.12 g, 161 mmol, 2 eq). The reaction medium is stirred at room temperature for 16 h. Excess L1AIH 4 is hydrolyzed by the addition of H 2 0 (4.2 mL) then with a 20% NaOH solution (3.4 mL) and H 2 0 (15.4mL). The precipitate is filtered and the filtrate is evaporated under vacuum. The residue obtained is purified by flash chromatography on silica gel using a mixture of heptane / AcOEt (70:30) as eluent. Intermediate 9 (8.09 g, 45.9 mmol) is obtained in the form of a colorless oil with a yield of 57%. Stage B5 (Intermediate 10): To a solution of intermediate 9 (8.09 g, 45.9 mmol) and CBr 4 (30.4 g, 91.8 mmol) at room temperature in Et 2 0 (325 mL) is added in portions of the triphenylphosphine (24.07 g, 91.8 mmol, 2 eq). The mixture is stirred for 16 h. The reaction medium is filtered and the filtrate is evaporated under vacuum. The residue is taken up in heptane (250 mL), stirred for 30 minutes and then filtered. The filtrate is evaporated under vacuum. The residue obtained is purified by flash chromatography on silica gel using heptane as eluent. Intermediate 10 (8.64 g, 36 mmol) is obtained in the form of a colorless oil with a yield of 78%. 1H NMR: (400 MHz, CDC1 3 ) δ ppm 7.28 (t, 2H), 7.18 (t, 1H), 7.13 (d, 2H), 5.53 (ddd, 1H), 5.02 (d, 1H), 5 (d, 1H) , 3.42 (m, 1H), 3.3 (m, 1H), 2.65 (d, 2H), 2.53 (m, 1H), 1.95 (m, 1H), 1.8 (m, 1H) IR Ccm 1 ): 916, 739-698 Stage B6 (Intermediate 11) To a solution of hypophosphorous acid (1.1 g, 16.7 mmol) in acetonitrile (25 mL) under Argon and at ambient temperature is added tetraethylorthosilicate (3.48 g, 16.7 mmol, 1 eq). The reaction mixture is heated at reflux for 2h30 and then cooled to room temperature. The reaction medium is degassed with argon, then intermediate 10 (2 g, 8.36 mmol) in solution in MeCN (5 mL), Xantphos (0.048 g, 0.0836 mmol) and then Pd are successively added. 2 dba 3 (0.038g, 0.0418mmol). The mixture is refluxed for 16 h. After evaporation under vacuum, the residue obtained is purified by flash chromatography on silica gel using AcOEt as eluent. Intermediate 11 (1.61 g, 4.85 mmol) is obtained in the form of an oil with a yield of 58%. 1H NMR: (400 MHz, dmso-d6) δ ppm centered at 6.95 (d, 1 H), 7.3 (t, 2 H), 7.2 (m, 3 H), 4 (m, 2 H), 3.55 (m , 2H), 2.59 (d, 2H), 1.9 (m, 1H), 1.78 (m, 4H), 1.45 (m, 2H), 1.21 (t, 3H) IR (cm 1 ): 2343 Intermediate B7 stage 12) A 1.06 M solution of LiHMDS in THF (4.53 mL , 4.8 mmol, 1 eq). The reaction medium is stirred for 30 minutes at −78° C. then 4 h 30 at room temperature before being treated with a saturated NaCl solution (50 mL). After addition of AcOEt (150 mL), the organic phase is dried over MgS0 4 then evaporated under vacuum. The residue obtained is purified by flash chromatography on silica gel using a DCM / EtOH (95:5) mixture as eluent. Intermediate 12 (0.889 g, 3.52 mmol) is obtained in the form of a colorless oil with a yield of 73%. 1H NMR: (400 MHz, CDC13) δ ppm 7.3 (t, 2 H), 7.2 (t, 1 H), 7.12 (d, 2 H), 4.08 (1 2.6 / 2.51 (2d, 2 H), 2.1- 1.8 (m, 4H), 1.8-1.55 (m, 3H), 1.5-1.3 (m+t, 5H) IR (cm 1 ): 3433 Stage B8 (Intermediate 13) To a solution of intermediate 12 (0.875 g, 3.47 mmol) in THF (10 mL) at -78°C and under Argon, is added a solution of 2M LDA in THF (2.6 mL, 5.2 mmol, 1.5 eq ). After 40 minutes, a solution of dibenzylcarbonate (1.18 g, 4.85 mmol) in THF (5 mL) is added dropwise. The reaction medium is stirred for 1 hour then 1.5 eq of 2M LDA in THF (2.6 mL, 5.2 mmol) are added. After 4 hours at -78°C, the reaction medium is cold hydrolyzed with an aqueous solution of NH 4 C1 10% (9mL). AcOEt (18 mL) and aqueous NH solution 4 C1 10%> (18 mL) are then added. After returning to ambient temperature, the reaction medium is extracted with AcOEt (2×50 mL). The organic phase is dried over MgS04 and then concentrated in vacuo. The residue obtained is purified by flash chromatography on silica gel using a DCM / EtOH (97.5:2.5) mixture as eluent. Intermediate 13 (0.996 g, 2.58 mmol) is obtained in the form of an oil with a yield of 74%. 1H NMR: (400 MHz, CDC13) δ ppm 7.4-7 (m, 10 H), 5.18 (s, 2 H), 4.15-3.9 (m, 2 H), 3.2-2.8 (1 dd, 1 H), 2.58 (d, 2H), 2.3-1.4 (m, 7H), 1.25 (t, 3H) IRJcm "1 ): 1726 Stage B9 (Intermediate 14) To a suspension of sodium hydride (0.150 g, 3.75 mmol, 1.6 eq) in DMSO (5 mL) are successively added dropwise a solution of intermediate 206 (1.11 g, 3.03 mmol, 1.3 eq) in DMSO (5 mL) and a solution of intermediate 13 (0.9 g, 2.33 mmol) in DMSO (4 mL). After 4 hours of stirring at room temperature, the reaction medium is added at 0° C. to a mixture (1:1) of a solution of NH 4 10% C1 (100 mL) and AcOEt (100 mL). The aqueous phase is re-extracted with AcOEt (2×50 mL). The organic phases are combined, dried over MgS0 4 then concentrated in vacuo. The intermediate 14 thus obtained is used directly without further purification. BIP stage (Intermediate 15 and 16) To a solution of intermediate 14 (1.56 g, 2.33 mmol) in DCM (125 mL) at ambient temperature and under argon, is added TMSBr (3.68 mL, 28 mmol, 12 eq). The reaction medium is stirred for 16 h at ambient temperature before being concentrated under vacuum. The oil obtained is taken up in MeOH (60 mL), stirred for 30 min and concentrated under vacuum. The same operation is repeated twice. The residue obtained is purified by reverse phase chromatography using an H gradient as eluent 2 0 / MeCN / TFA. Intermediates 15 (0.423 g, 0.95 mmol) then 16 (0.155 g, 0.35 mmol) (in the order of elution) are obtained in the form of white solids after lyophilization with respective yields of 41% and 15%. The absolute configuration of intermediates 15 and 16 has not been verified. Intermediate 15: Benzyl 2-(5-Aminopentyl)-4-benzyl-l-hydroxy-l-oxo-l-phosphinane-2-carboxylate, trifluoroacetate - racemic dia 1 1H NMR: (400 MHz, dmso-d6) δ ppm 12 (m, 1H), 7.75 (m, 3H), 7.35-7.05 (m, 10H), 5.18 / 5 (2d, 2H), 2.6 (m, 3H), 2.4 (dd, 1H), 2.1 (m, 1H), 1.9-1.5 (m, 8H), 1.4 (m, 2H), 1.15 (m, 2H), 0.8 / 0.52 (2m, 2H) NMR 19 F: (400 MHz, dmso-d6) δ ppm -74 IR (cm 1 ): 3300-2500, 1716, 1678 Intermediate 16: Benzyl 2-(5-Aminopentyl)-4-benzyl-l-hydroxy-l-oxo-l-phosphinane-2-carboxylate, trifluoroacetate - racemic dia 2 1H NMR (400 MHz, dmso-d6) δ ppm 7.4 (m, 5 H), 7.25 (t, 2 H), 7.18 (t, 1 H), 7 (d, 2 H), centered at 5.11 (AB, 2H), 7.65 (m, 3H), 2.71 (m, 2H), 2.4 (d, 2H), 1.95-1.1 (m, 15H) NMR 19 F: (400 MHz, dmso-d6) δ ppm -74 IRcm "1 ): 3300-2500, 1774, 1716, 1676 EXAMPLE 20: 2-(5-Aminopentyl)-4-benzyl-l-hydroxy-l-oxo-l-phosphinan-2-carboxylic acid, racemic dia 1 Intermediate 15 (0.413g, 0.74 mmol) in solution in 60 mL of a mixture (3: 1) H 2 0 / MeOH is stirred at room temperature under an atmosphere of H 2 , in the presence of Pd 10% / C (41mg) for 4h. The reaction medium is filtered and then concentrated under vacuum. The residue obtained is purified by reverse phase chromatography using a gradient as eluent H 2 0 / MeCN. Example 20 (0.209 g, 0.591 mmol) is obtained in the form of a white solid after lyophilization with a yield of 80%. 1H NMR: (500 MHz, D20) δ ppm 7.3 (t, 2 H), 7.24 (d, 2 H), 7.19 (t, 1 H), 2.59 / 2.37 (m, 2 H), 2.41 (t, 2H), 1.91 / 1.55 ​​(m, 2H), 1.77 / 1.6 (m, 2H), 1.77 / 1.35 (m, 2H), 1.64 / 1.38 (m, 2 H), 1.63 (m, 1H), 1.24 (m, 2H), 1.16 / 1.1 (m, 2H), 0.7 (m, 2H) NMR 13 C: (500 MHz, D20) δ ppm 129.2, 128.2, 125.7, 42.5, 40, 35.5, 35.4, 31.3, 31.1, 30.2, 26, 25.9, 22.8 IR (cm 1 ): 3300-2100, 1691, 1631, 1605 Elemental Analysis: C=60.65(61.18);H=7.58(7.99);N=3.91(3.96) ESI / FIA / HR and MS / MS: [M+H]+ = 354.1831 (354.1834) EXAMPLE 21: 2-(5-Aminopentyl)-4-benzyl-l-hydroxy-l-oxo-l-phosphinan-2-carboxylic acid, racemic dia 2 Intermediate 16 (0.148 g, 0.265 mmol) in solution in 20 mL of a mixture (3: 1) H 2 0 / MeOH is stirred at room temperature under an atmosphere of H 2 , in the presence of 10% Pd / C (15 mg) for 2h30. The reaction medium is filtered and then concentrated under vacuum. The residue obtained is purified by reverse phase chromatography using an H gradient as eluent 2 0 / MeCN. Example 21 (0.053 g, 0.15 mmol) is obtained in the form of a white solid after lyophilization with a yield of 56%. 1H NMR: (500 MHz, D20) δ ppm 7.29 (t, 2 H), 7.2 (d, 2 H), 7.2 (t, 1 H), 2.57 (t, 2 H), 2.45 (m, 2 H) , 1.84 (m, 1H), 1.81 / 1.33 (m)+(m, 1+1H), 1.78 / 1.29 (m)+(m, 1+1H), 1.69 / 1.31 (m)+(m , 1+1H), 1.68 / 1.27 (m)+(m, 1+1H), 1.41 / 1.19 (m)+(m, 1+1H), 1.38 (m, 2H), 1.2 (m , 2H) NMR 13 C: (500MHz, D 2 0) δ ppm 129.3, 128.2, 125.7, 43, 42.4, 40, 35.9, 34.6, 30.4, 29.4, 27, 26.7, 25 IR (cm 1 ): 3250-1800, 1694+1661, 1618 Elemental Analysis: C=61.18(61.18);H=7.90(7.99);N=3.96(3.96) ESI / FIA / HR and MS / MS: [M+H]+ = 354.1837 (354.1834) In the same way, examples 22 and 23 are obtained according to procedure B previously described by replacing intermediate 206 with intermediate 204. EXAMPLE 22: Acid 2-(4-aminobutyl)-4-benzyl-1-hydroxy- l-oxo-l-phosphinane-2- carboxylic, racemic dia 1 1H NMR: (400 MHz, dmso-d6) δ ppm 7.7 (si, 3H), 7.3 (dd, 2H), 7.2 (dd+t, 3H), 2.7 (m, 2H), 2.55-2.4 (m, 2H), 1.95 (m, 1H), 1.8-13 (m, 10H), 1.1-0.85 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 340.1677 (340.1677) Elemental Analysis: C=51.00(50.33);H=5.90(6.00);N=3.22(3.09) EXAMPLE 23: 2-(4-Aminobutyl)-4-benzyl-l-hydroxy-l-oxo-l-phosphinane-2-carboxylic acid, dia 2 racemic 1H NMR: (300 MHz, dmso-d6) δ ppm 15.8 (m, 2 H), 7.95 (m, 2 H), 7.25 (t, 2 H), 7.18 (t, 1 H), 7.1 (d, 2 H), 2.75 (m, 2H), 2.6-2.35 (m, 2H), 2.15 (m, 1H), 1.75-1 (m, 12H) ESI / FIA / HR and MS / MS: [M+H]+ = 340.1683 (340.1677) Elemental Analysis: C=60.20(60.17);H=7.34(7.72);N=3.96(4.13) Synthesis of azaphosphinanes Intermediate 17 Intermediate 17 was synthesized using a procedure described in the literature by V. Gouverneur et al., J. Org. Chem. 2005, 70, 10803. To a solution of ethyl dichlorophosphinate (10 mL, 84.26 mmol) in 100 mL of THF at -78°C and under Argon, is added a 1M solution in THF of vinyl magnesium bromide (170 mL, 170 mmol, 2 eq). Stirring is maintained for lh at -78°C. EtOH (30 mL) is then added dropwise and the reaction is brought back to room temperature. The reaction medium is then concentrated under reduced pressure and the residue obtained is purified by flash chromatography on silica gel using a DCM / EtOH (96:4) mixture as eluent. Intermediate 17 (6.37 g, 43.6 mmol) is obtained in the form of a colorless oil with a yield of 52%. 1H NMR: (400 MHz, DMSO - d 6 ) δ 6.1-6.4 (m, 6H), δ 3.90 (q, 2H), δ 1.25 (t, 3H). IR (cm 1 ): 3500 (OH(H 2 0)), 1609 (C=C), 1210 (P=0), 1032 and 935 cm "1 (P-O). GC: t r 5.83 mins. Intermediate 18 N-benzylamine (4.79 mL, 43.6 mmol, 1 eq.) is added all at once to a solution of intermediate 17 (6.37 g, 43.6 mmol) in an autoclave and under Argon. The mixture reaction is heated to 100° C., stirred for 16 h and concentrated under reduced pressure. The residue is taken up with AcOEt (100 mL), the organic phase is washed with a saturated NaCl solution (3 x 100 mL) and dried with MgS0 4 . The solvent is evaporated off and the residue obtained is purified by flash chromatography on silica gel using a DCM / EtOH (95:5) mixture as eluent. Intermediate 18 (8.68 g, 34.3 mmol) is obtained in the form of a yellowish oil with a yield of 79%. 1H NMR: (CDC1 3 , 400 MHz) δ 7.31 (m, 5H), 4.08 (m, 2H), 3.60 (s, 2H), 2.98 (m, 2H), 2.64 (m, 2H), 1.97 (m, 2H), 1.85 (m , 2H), 1.35 (t, 3H). GC: t r 12.29 mins. Intermediate 19 To a solution of intermediate 18 (6.38 g, 25.19 mmol) in THF (30 mL) at -70°C and under Argon, is added a solution of LDA (75.6 mL, 37.8 mmol, 1.5 eq) at 2M in the THF. After 15 min at -70°C, a solution of Boc 2 0 (7.68 g, 35.3 mmol, 1.4 eq) in 30 mL of THF is then added dropwise. Stirring is maintained for 90 min and 1.5 eq of LDA (75.6 mL, 37.8 mmol) are then added drop by drop. At the end of the addition, the reaction medium is maintained at -70° C. for 90 min. A saturated solution of NH 4 CI (30 mL) as well as AcOEt (60 mL) are added and the reaction medium is slowly brought back to room temperature. The product is then extracted with AcOEt (2 x 150 mL). The organic phases are combined, washed with a saturated NaCl solution (2 x 150 mL), dried over MgS0 4 and concentrated under reduced pressure. The residue obtained is purified by flash chromatography on silica gel using a gradient of DCM / THF (95:5 to 40:60) as eluent. Intermediate 19 (6.73 g, 19.04 mmol) is obtained in the form of a yellowish oil with a yield of 76%. 1H NMR: (CDCI3, 400 MHz) δ 7.35 to 7.2 (m, 5H), δ 4.3 to 4.05 (m, 2H), δ 3.60 (dd, 2H), δ 3.3 to 2.5 (m, 5H), δ 2.1 to 1.8 (m, 2H), δ 1.50 (s, 9H), δ 1.35 (t, 3H). IR (cm 1 ): 3500 (OH), 1721 (C=0), 1150 (P=0), 1032 and 935 (P-O). MS_^ m / z 355 [M+1]. Procedure C: Intermediate 19 Alkylation Procedure To a solution of intermediate 204 to 212 (5 mmol, 1 eq) in DMSO (10 mL) under Argon, is added NaH at 60% (8 mmol, 1.6 eq) in portions at 10°C. Intermediate 19 (5 mmol) in solution in DMSO (5 mL) is then added to the suspension and the mixture is stirred for 4 hours at ambient temperature. The reaction medium is then hydrolyzed with an aqueous solution of NH 4 C1 (50 mL) and extracted with AcOEt (2 x 100 mL). The organic phase is washed with H 2 0 (2 x 100 mL), dried over MgS0 4 and concentrated in vacuo. The residue obtained is purified by flash chromatography on silica gel using a DCM / AcOEt (90:10 to 50:50) gradient as eluent. Intermediate 20a-f is obtained in the form of a mixture of 4 diastereoisomers. Procedure D: Deprotection of amino and phosphinic functions TMSBr (7.92 mL, 60 mmol, 12 eq) is added dropwise to a solution of intermediate 20a-f (5 mmol) in DCM (40 mL) under Argon and at ambient temperature. The mixture is stirred for 16 h at room temperature and then concentrated under vacuum. The residue is taken up in MeOH (40 mL) and stirred for 20 min at room temperature before being evaporated to dryness. The evaporate is dissolved in DCM (20 mL) and trifluoroacetic acid (44.6 mL, 60 mmol, 12 eq) is added. The reaction medium is stirred for 1 Oh at room temperature and then concentrated under vacuum. The residue obtained is purified by reverse phase chromatography using an H gradient as eluent 2 0 / MeCN. The final product (Examples 24 to 30) (zwitterion or TFA salt), mixture of 2 enantiomers, is obtained in the form of a white solid after lyophilization. Intermediate 20a: tert-Butyl 3-{3-[Bis(terf-butoxycarbonyl)amino]propyl}-1-benzyl-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 20a is obtained from intermediates 19 and 205 according to procedure C previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.35-7.2 (m, 5H), 4 (m, 2H), 3.8 (m, 2H), centered at 3.52 (AB, 2H), 3 -2.25 (m, 4H), 2-1.8 (m, 4H), 1.45 / 1.35 (2s, 27H), 1.2 (t, 3H), 1.2 (m, 2H) EXAMPLE 24: 3-(3-Aminopropyl)-1-benzyl-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 24 is obtained from intermediate 20a according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.5 (m, 5 H), centered at 4.35 (AB, 2 H), 3.75 / 3.35 (2m, 2 H), 3.5 / 3.15 (2dd, 2 H), 2.92 (t, 2H), 2.3 / 1.8 (2m, 2H), 1.95 (m, 1H), 1.6-1.4 (m, 3H) ESI / FIA / HR and MS / MS: [M+H]+ = 327.1478 (327.1473) Elemental Analysis: C=55.38(55.21);H=6.85(7.10);N=8.41(8.58) Intermediate 20b: tert-butyl 3-{4[Bis(terf-butoxycarbonyl)amino]butyl}-1-benzyl-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 20b is obtained from intermediates 19 and 204 according to procedure C previously described. 1H NMR: (DMSO-dg, 400 MHz) δ 7.30 (m, 5H), 3.97 (m, 2H), 3.63-3.43 (dd, 2H), 3.36 (m, 2H), 2.93-2.33 ( m, 2H), 2.79 to 2.47 (m, 2H), 1.93 (m, 2H), 1.93 (m, 2H), 1.43 (m, 2H), 1.42 (s, 18H), 1.36 ( s, 9H), 1.21 (t, 3H), 0.83 (m, 2H). IR (cm 1 ): 1744, 1711cm "1 (C=0), 1276cm "1 (P=0). EXAMPLE 25: 3-(4-Aminobutyl)-1-benzyl-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 25 is obtained according to procedure D previously described from intermediate 20b. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.2 (si, 3 H), 7.3 (m, 5 H), 3.7 / 3.5 (2*(d, 1+1 H), 3.05 / 2.4 (2* (m, 1+1H), 2.75 / 2.55 (2*(m, 1+1H), 2.7 (m, 2H), 1.8 (m, 1H), 1.6-1.1 (m, 7H) ESI / FIA / HR and MS / MS: [M+H]+ = 341.1628 (341.1630) Elemental Analysis: C=55.99(56.46);H=7.14(7.40);N=8.13(8.23) Intermediate 20c: 3-{5-Bis(tert-butoxycarbonyl)amino]pentyl}-l-benzyl-4-ethoxy- tert-Butyl 4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 20c is obtained from intermediates 19 and 206 according to procedure C previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.32-7.2 (m, 5H), 3.99 (m, 2H), 3.8 (m, 2H), centered at 3.5 (AB, 2H), 3 -2.3 (m, 4H), 2-1.8 (m, 4H), 1.45 / 1.35 (2s, 27H), 1.35 / 1.15 (2m, 4H), 1.2 (t, 3H), 0.75 (m , 2H) EXAMPLE 26: 3-(5-Aminopentyl)-1-benzyl-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 26 is obtained from intermediate 20c according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.5 (m, 5 H), centered at 4.32 (AB, 2 H), 3.7 / 3.35 (2m, 2 H), 3.5 / 3.1 (2dd, 2 H), 2.9 (t, 2H), 2.2 / 1.78 (2m, 2H), 1.95 / 1.45 (2m, 2H), 1.6 (m, 2H), 1.3 (m, 2H), 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 355.1792 (355.1786) Elemental Analysis: C=58.04(57.62);H=7.37(7.68);N=7.95(7.90) Intermediate 20d: 1-Benzyl-3-({6-[bis-terf-butoxycarbonyl)amino]pyridin-3-yl tert-Butyl}methyl)-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 20d is obtained from intermediates 19 and 211 according to procedure C previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.18 (s, 1H), 7.4-7.25 (m, 6H), 7.18 (d, 1H), 4 (m, 2H), 3.8 (m , 2H), 3.58 / 3.5 (2d, 2H), 3-2.6 (m, 4H), 2.25 / 2.1 (2m, 2H), 1.4 (s, 27H), 1.2 (t, 3H) EXAMPLE 27: 3-[(6-aminopyridin-3-yl)methyl]-l-benzyl-4-hydroxy-4-azaphosphinane-3-carboxylic acid Example 27 is obtained from intermediate 20d according to the procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.51 (dd, 1 H), 7.42 (d, 1 H), 7.4-7.25 (m, 5 H), 6.75 (d, 1 H), centered at 4.25 (AB , 2H), 3.78 (m, 1H), 3.4 (dd+m, 2H), 2.95 (dd, 1H), 2.7 (dd, 1H), 2.6 (dd, 1H), 2.28 / 1.85 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 376.1418 (376.1426) Elemental Analysis: C=57.18(57.60);H=5.82(5.91);N=11.25(11.19) EXAMPLE 28: 3-[(2-Aminopyridin-4-yl)methyl]-1-benzyl-4-hydroxy-4-oxo-1,4-azaphosphinan-3-carboxylic acid Example 28 is obtained from intermediates 19 and 212 according to procedures C and D previously described without intermediate purification. 1H NMR: (400 MHz, D20) δ ppm 7.6 (dl, 1H), 7.4 (m, 5H), 6.55 (m, 2H), 4.6 / 4 (dd, 2H), 3.9-3.4 (m , 2H), 3.6 / 2.75 (dd, 2H), 3 / 2.7 (dd, 2H), 2.3 / 1.9 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 376.1428 (376.1426) Elemental Analysis: C=56.70(57.60);H=5.45(5.91);N=10.87(11.19) Intermediate 20e: tert. -butyl Intermediate 20e is obtained from intermediates 19 and 208 according to procedure C previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.4-7.3 (m, 5H), 7.15 (t, 1H), 7.1 (si, 1H), 7.05 / 6.95 (d, 2H), 4.6 (s, 2 hrs), 4 (m, 2 hrs), 3.7 / 3.45 (dd, 2 hrs), 3.35 (m, 2 hrs), 2.9 / 2.15 (m, 2 hrs), 2.7 / 2.55 (dd, 2 H), 2.05 (m, 2H), 1.4 (s, 27H), 1.2 (t, 3H) EXAMPLE 29: 3-[[3-(aminomethyl)phenyl]methyl]-1-benzyl-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 29 is obtained from intermediate 20e according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.3 (m, 5H), 7.3-7.05 (m, 4H), 4.4 / 3.95 (dd, 2H), 4 (dd, 2H), 3.8-3.3 (m, 2H), 3.55 / 2.75 (dd, 2H), 3 / 2.7 (dd, 2H), 2.2 / 1.8 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 389.1623 (389.1630) Elemental Analysis: C=61.37(61.85);H=6.30(6.49);N=7.05(7.21) Intermediate 20f: tert-1-Benzyl-3-(4-{[bis(tei"i-butoxycarbonyl)amino]methyl)}benzyl)-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate butyl Intermediate 20f is obtained from intermediates 19 and 209 according to procedure C previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.35 (m, 5H), 6.99 (d, 2H), 6.91 (d, 2H), 4.6 (s, 2H), 3.98 (m, 2 H), 3.5 (s, 2H), 3.27 (m, 2H), 2.95 / 2.22 (2*m, 2H), 2.75 / 2.49 (2*m, 2H), 2.05 (m, 2H) , 1.35 (2*s, 27H), 1.18 (t, 3H) NMR 13 C: (400 MHz, dmso-d6) δ ppm 152, 138, 137, 135, 130, 128, 126, 82, 62, 60, 55.5, 50.5, 48.5, 34, 28, 24.5, 16 EXAMPLE 30: Acid 3 -[[4-(aminomethyl)phenyl]methyl]-l-benzyl-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic Example 30 is obtained from intermediate 20f according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.2 (m, 5H), 7.1 / 7 (dd, 4H), 4.3 / 3.9 (dd, 2H), 4 (m, 2H), 3.7-3.25 (m, 2H), 3.45 / 2.65 (dd, 2H), 2.9 / 2.65 (dd, 2H), 2.15 / 1.75 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 389.1623 (389.1630) Elemental Analysis: C=61.41(61.85);H=6.36(6.49);N=7.40(7.21) Intermediate 20b: tert-butyl 3-{4[Bis(terf-butoxycarbonyl)amino]butyl}-1-benzyl-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate In a three-necked IL flask equipped with a mechanical stirrer are successively introduced under an argon atmosphere of DMSO (30 mL) and 60% NaH (8.48 g, 212 mmol, 1.5 eq). The flask is maintained at room temperature using a water bath. A solution of intermediate 204 (54.6 g, 155 mmol, 1.1 eq) in DMSO (25 mL) is then added dropwise over a period of 5 minutes. A solution of intermediate 19 (50 g, 141.5 mmol) in DMSO (120 mL) is then added dropwise while maintaining the temperature below 20°C. After the end of the addition, 100 mL of anhydrous THF are then added in order to be able to maintain stirring. After 3 hours, the reaction mixture is cooled using an ice water bath and hydrolyzed by adding 500 mL of a solution saturated with NH 4 C1. The mixture is then extracted with AcOEt (3 x 300 mL). The organic phases are then combined, washed with a saturated NaCl solution (2×300 mL), and dried over MgSC 4 before being concentrated under reduced pressure. The yellowish residue (92.5 g) thus obtained is then purified by chromatography on silica gel using a CH 2 Cl 2 / AcOEt / MeOH as eluent. The expected product (69.3 g, 110.9 mmol), mixture of 4 diastereoisomers, is obtained in the form of a white solid with a yield of 78%. Procedure E: Procedure debenzylation by hydrogenolysis Intermediate 21: tert-butyl 3-{4-[Bis(tert-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate In a 2L flask at room temperature and under argon flow, intermediate 20b (73.6 g, 117.8 mmol), ethanol (1 L), Pd / C (7.36 g, 10% by weight) and 37% HCl (7.85 mL) are successively introduced. , 0.8 eq). The argon is then replaced by an atmosphere of hydrogen. The reaction is followed by LC / MS. After 4 hours, the reaction is complete and the catalyst is filtered through fiberglass. The filtrate is evaporated to dryness in order to obtain a yellow oil which is taken up in AcOEt (400 mL) and in a solution of NaHC0 3 at 10% > (400 mL). After decantation, the aqueous phase is extracted with AcOEt (3×100 mL). The organic phases are combined then washed with a saturated NaCl solution (400 mL), dried over MgSC^ and concentrated to yield the expected intermediate 21 in the form of a white solid (57.6 g, 107.7 mmol) with a yield of 91%. 1H NMR: (DMSO-dg, 400 MHz) δ 4.05 to 3.85 (m, 2H), 3.45 (m, 2H), 3.1 to 2.6 (m, 4H), 2.3 -1.7 (m, 4H), 1.45 (s, 18H), 1.40 (s, 9H), 1.20 (t, 3H), 1.5-0.9 (m, 4H). IRcm "1 ): 3100-3500 cm ^OH), 3314 cm "1 (NH), 1712-1693cm "1 (C=0). Procedure L: Procedure for the synthesis of Ar aldehydes 2 -Ari-CHO by a Suzuki coupling The non-commercial aldehydes were prepared according to the procedure described below: In a 1 L flask under argon at room temperature are successively introduced ethanol (500 mL), boronic acid Ar 2 -B(OH) 2 (92.7 mmol, 1.2 eq) and bromoarylaldehyde or bromoheteroarylaldehyde Br-Ari-CHO (77.3 mmol). The solution is degassed with Argon for 15 min. Pd(PPh 3 ) 4 (1.78 g, 1.55 mmol) and Na 2 C0 3 (92.7 mL of a 2M solution in H 2 0.185 mmol, 2.4 eq) are then introduced in one portion. After the addition, the reaction mixture is refluxed for 5 hours. The medium is then evaporated to dryness. The residue is taken up with DCM (1 L) and H 2 0 (200mL). After decantation, the aqueous phase is extracted with DCM (200 mL). The organic phases are combined then washed with a saturated NaCl solution (400 mL), dried over MgS0 4 and concentrated under reduced pressure. The residue is then purified by flash chromatography on silica gel. The expected product is obtained with yields of 59 to 94%. Intermediate 213 1H NMR: (400 MHz, dmso-d6) δ ppm 9.89 (s, 1H), 7.94 (dd, 1H), 7.77 (td, 1H), 7.63 (tl, 1H), 7.54 (dl, 1 H), 7.54 / 7.4 (2m, 4H) Intermediate 214 1H NMR: (400 / 500 MHz, dmso-d6) δ ppm 9.72 (s, 1H), 7.96 (d, 1H), 7.79 (t, 1H), 7.65 (t, 1H), 7.6 (t , 1H), 7.48 (m, 3H), 7.4 (d, 1H) Intermediate 215 1H NMR: (400 / 500 MHz, dmso-d6) δ ppm 9.91 (s, 1H), 7.95 (d, 1H), 7.78 (m, 1H), 7.78 (m, 1H), 7.74 (d , 1H), 7.64 (t, 1H), 7.53 (d, 1H), 7.44 (dd, 1H) IED (70eV: [M]+.=250 Intermediate 216 1H NMR: (400 MHz, dmso-d6) δ ppm 9.59 (s, 1H), 9.43 (s, 1H), 8.46 (d, 1H), 8.26 (d, 1H), 8.06 (d, 1 H), 7.85 (t, 1H), 7.81 (t, 1H), 7.77 (d, 1H), 7.74 (t, 1H), 7.51 (d, 1H), 7.24 (d, 1H) Intermediate 217 1H NMR: (400 MHz, CDC13) δ ppm 9.2 (s, 1 H), 8.1 (dd, 1 H), 7.85 (m, 2 H), 7.4 (m, 2 H), 7.3 (dd+s, 2 H), 7.2 (td, 1H) NMR 19 F: (400 MHz, CDC13) δ ppm -101.1 GC-EI (70eV: [M]+. = 256 Intermediate 218 1H NMR: (400 MHz, dmso-d6) δ ppm 9.25 (s, 1H), 8.8 (d, 1H), 8 (m, 1H), 7.85 (m, 1H), 7.85 / 7.75 (2m , 2H), 7.05 (d, 1H) Intermediate 219 1H NMR: (400 MHz, dmso-d6) δ ppm 10.05 (s, 1H), 9.2 (s, 1H), 8.05 (m, 2H), 7.7 (m, 3H) Intermediate 220 NMR Ή: (400 MHz, dmso-d6) δ ppm 9.81 (s, 1H), 8.02 (dd, 1H), 7.58 / 7.52 (2d, 4H), 7.46 (td, 1H), 7.4 (dd , 1H) GC-EI (70eV: [M]+. = 234 Intermediate 221 NMR Ή: (400 MHz, dmso-d6) δ ppm 9.82 (s, 1H), 7.97 (dd, 1H), 7.42 (d, 2H), 7.38 (td, 1H), 7.35 (dd, 1 H), 7.09 (d, 2H), 3.83 (s, 3H) Intermediate 222 NMR Ή: (400 MHz, dmso-d6) δ ppm 9.82 (s, 1H), 7.99 (dd, 1H), 7.42 (m, 3H), 7.08 / 7.01 (2dl, 2H), 7.06 (si , 1H), 3.82 (s, 3H) Intermediate 223 NMR Ή: (400 MHz, dmso-d6) δ ppm 9.9 (s, 1H), 7.92 (dd, 1H), 7.78 (td, 1H), 7.69 (dd, 1H), 7.65 (dd, 1 H), 7.38 (d, 1H), 7.07 (d, 1H), 3.68 (s, 3H) Intermediate 224 1H NMR: (400 MHz, dmso-d6) δ ppm 9.8 (si, 1 H), 7.68 (dd, 1 H), 7.62 (m, 2 H), 7.54 (m, 3 H), 7.5 (d, 1H) GC-EI (70eV: [M]+. = 188 Intermediate 225 1H NMR: (400 MHz, dmso-d6) δ ppm 10.35 (s, 1H), 8.07 (d, 1H), 7.99 (d, 1H), 7.88 (m, 2H), 7.79 / 7.67 (2 *t, 2H) Intermediate 226 1H NMR: (400 MHz, dmso-d6) δ ppm 9.9 (s, 1H), 7.95 (d, 1H), 7.8 (m, 1H), 7.65 (m, 1H), 7.5 (d, 1 H), 6.85 (s, 1H), 3.4 (s, 3H), 2.4 (s, 3H) Intermediate 227 1H NMR: (400 MHz, dmso-d6) δ ppm 9.85 (s, 1H), 8.15 (m, 1H), 8.06 (m, 1H), 7.85 (m, 1H), 7.74 (s, 1 H), 7.7 (m, 1H), 7.7 (m, 1H), 7.7 (m, 1H), 7.35 (m, 1H), 6.95 (m, 1H) Intermediate 228 1H NMR: (400 / 500 MHz, dmso-d6) δ ppm 9.53 (s, 1H), 8.08 (d, 1H), 8.08 (d, 1H), 8.02 (dd, 1H), 7.83 (td , 1H), 7.71 (tt, 1H), 7.63 (dd, 1H), 7.57 (td, 1H), 7.51 (d, 1H), 7.49 (d, 1H), 7.49 (td, 1 H), 7.38 (dt, 1H) NMR 13 C: (400 / 500 MHz, dmso-d6) δ ppm 192, 143.5, 135.5, 135, 134, 133, 132, 128.5, 128.5, 128, 128, 127, 127, 126.5, 125.5, 125 Intermediate 229 1H NMR: (400 MHz, CDC13) δ ppm 9.9 (s, 1H), 8.05 (dd, 1H), 7.15 (m, 2H), 7 (d, 1H), 6.9 (m, 2H) , 3.95 (2s, 6H) IED (70eV: [M]+.=260 Intermediate 230 1H NMR: (400 MHz, dmso-d6) δ ppm 10.8 (si, 1 H), 9.7 (s, 1 H), 8.2 (d, 1 H), 7.83 (d, 1 H), 7.79 (dd, 1 H), 6.95 (dd, 1H), 6.91 (d, 1H), 6.77 (d, 1H), 3.9 (s, 3H) Intermediate 231 NMR Ή: (400 MHz, CDC13) δ ppm 10.2 (s, 1 H), 8 (dd, 1 H), 7.75 (t, 1 H), 7.4 (dd, 1 H), 7.2 (m, 2 H) , 6.8 (d, 1H), 3.95 (s, 3H) GC-EI (70eV): [M]+. = 231 Intermediate 232 NMR Ή: (400 MHz, CDC13) δ ppm 10.5 (m, 1 H), 8.1 (dd, 1 H), 8 (m, 1 H), 7.5 (d, 1 H), 7.4 (dd, 1 H) , 7.25 (td, 1H) GC-EI (70eV^: [M]+. = 207 Intermediate 233 1H NMR: (400 MHz, dmso-d6) δ ppm 10 (s, 1H), 8.65 (s, 1H), 8.06 (m, 2H), 7.6 (m, 3H) Intermediate 234 1H NMR: (400 MHz, CDC13) δ ppm 9.8 (s, 1H), 8.2 (dd, 1H), 8 (d, 1H), 7.8 (d, 1H), 7.75 (s, 1H) , 7.3 (m, 3H), 6.95 (t, 1H) GC-EI (70eV): [M]+. = 240 Intermediate 235 1H NMR: (400 MHz, dmso-d6) δ ppm 10.15 (d, 1H), 8.05 (s, 1H), 7.86 (dd, 1H), 7.7 (d, 1H), 7.68 (td, 1 H), 7.53 (dd, 1H), 7.46 (td, 1H), 3.91 (s, 3H) Intermediate 236 1H NMR: (400 MHz, dmso-d6) δ ppm 10 (s, 1H), 9.25 (s, 1H), 8.91 (s, 2H), 8.05 (dd, 1H), 7.83 (td, 1 H), 7.73 (td, 1H), 7.58 (dd, 1H) Intermediate 237 1H NMR: (300 MHz, dmso-d6) δ ppm 9.9 (s, 1H), 8.25 (s, 1H), 7.95 (d, 1H), 7.85 (dd, 1H), 7.75 / 7.6 (2 *m, 2H), 7.55 (d, 1H), 6.95 (d, 1H), 3.9 (s, 3H) Intermediate 238 1H NMR: (400 / 500 MHz, dmso-d6) δ ppm 9.64 (s, 1H), 7.68 (d, 1H), 7.63 (t, 1H), 7.57 (t, 1H), 7.51 (t , 1H), 7.47 (d, 1H), 7.45 (t, 1H), 7.42 (d, 1H), 7.34 (d, 1H), 7.17 / 7.03 (2*m, 5H) Intermediate 239 1H NMR: (400 MHz, dmso-d6) δ ppm 9.8 (s, 1H), 8 (d, 1H), 7.8 (t, 1H), 7.69 (t, 1H), 7.6 (d, 1 H), 7.55 (m, 2H), 7.4 (d, 1H) GC-EI (70eV: [M]+. = 250 Intermediate 240 1H NMR: (400 / 500 MHz, dmso-d6) δ ppm 9.95 (s, 1H), 8.07 (d, 1H), 8.02 (m, 2H), 7.99 (d, 1H), 7.98 (dd , 1H), 7.8 (td, 1H), 7.64 (d, 1H), 7.62 (td, 1H), 7.62 (m, 1H), 7.6 (m, 2H) NMR 13 C: (400 / 500 MHz, dmso-d6) δ ppm 192, 134, 131.5, 129, 128, 128, 128, 128, 127.5, 127 Intermediate 241 1H NMR: (400 / 500 MHz, dmso-d6) δ ppm 9.98 (s, 1H), 7.95 (dd, 1H), 7.78 (m, 1H), 7.78 (m, 1H), 7.75 (d , 2H), 7.72 (t, 1H), 7.63 (d, 1H), 7.62 (t, 1H), 7.61 (t, 1H), 7.49 (t, 2H), 7.44 (dt, 1 H), 7.4 (t, 1H) NMR 13 C: (400 / 500 MHz, dmso-d6) δ ppm 192, 145.5, 140, 134, 133.5, 131, 129, 129, 128, 128, 128, 127.5, 127, 127, 127 Intermediate 242 1H NMR: (400 MHz, dmso-d6) δ ppm 9.77 (s, 1H), 8.05 (dd, 1H), 7.82 (td, 1H), 7.7 (td, 1H), 7.6 (d, 2 H), 7.5 (t, 1H), 7.35 (dd, 1H) Intermediate 243 1H NMR: (400 MHz, dmso-d6) δ ppm 9.9 (s, 1H), 9.25 (s, 1H), 8.95 (s, 2H), 8.15 (dd, 1H), 7.55 (m, 2 H) NMR 19 F: (400 MHz, dmso-d6) δ ppm -102.8 Intermediate 244 1H NMR: (400 MHz, CDC13) δ ppm 10 (s, 1 H), 8.25 (dd, 1 H), 8.05 (dd, 1 H), 7.7 (td, 1 H), 7.55 (td, 1 H) , 7.4 (dd, 1H), 6.9 (dd, 1H), 6.75 (dd, 1H), 4 (s, 3H) Intermediate 245 1H NMR: (400 MHz, dmso-d6) δ ppm 9.7 (s, 1H), 7.9 (dd, 1H), 7.75 (td, 1H), 7.58 (t, 1H), 7.43 (d, 1 H), 7.25-7.15 (m, 2H), 6.91 (dd, 1H), 3.87 (s, 3H), 3.38 (s, 3H) Intermediate 246 1H NMR: (300 / 400 / 500 MHz, dmso-d6) δ ppm 10.03 (s, 1H), 7.98 (dd, 1H), 7.83 (dd, 1H), 7.46 (dd, 1H), 7.43 (td, 1H), 7.36 (dd, 1H), 7.25 (dd, 1H) NMR 13 C: (300 / 400 / 500 MHz, dmso-d6) δ ppm 190.2, 165, 140.3, 137.3, 131.2, 130.7, 130.6, 129, 128.4, 117.8, 115.9 NMR 19 F: (300 / 400 / 500 MHz, dmso-d6) δ ppm -103 Intermediate 247 1H NMR: (300 / 400 / 500 MHz, dmso-d6) δ ppm 9.9 (s, 1H), 8.06 (s, 1H), 8.05 (d, 1H), 8.04- 8.02 (m, 3H) , 7.64 (dd, 1H), 7.61 (td, 2H), 7.51-7.47 (m, 2H) NMR 13 C: (300 / 400 / 500 MHz, dmso-d6) δ ppm 190.4, 165, 148.3, 131.2, 130.6, 129.5-128.2, 128.2, 127.7, 127.1, 117.9 / 115.5 NMR 19 F: (300 / 400 / 500 MHz, dmso-d6) δ ppm -103.2 Intermediate 248 1H NMR: (400 MHz, CDC13) δ ppm 9.88 (s, 1H), 8.1 (dd, 1H), 7.74 (s, 1H), 7.29 (td, 1H), 7.14 (s, 1H) , 7.1 (dd, 1H), 3.56 (s, 3H) Intermediate 249 1H NMR: (400 MHz, dmso-d6) δ ppm 9.84 (s, 1H), 8.27 (d, 1H), 8.04 (dd, 1H), 7.5 (td, 1H), 7.43 (dd, 1 H), 7.1 (dd, 1H), 6.96 (s, 1H), 3.91 (s, 3H) NMR 19 F: (400 MHz, CDC13) δ ppm -101.2 Intermediate 250 1H NMR: (400 MHz, dmso-d6) δ ppm 10.1 (s, 1H), 8.12 (d, 1H), 7.93 (d, 1H), 7.78 (dd, 1H), 7.39 (dd, 1 H), 7.3 (td, 1H), 3.91 (s, 3H) Intermediate 251 1H NMR: (400 MHz, dmso-d6) δ ppm 9.76 (s, 1H), 7.98 (dd, 1H), 7.79 (td, 1H), 7.77 (d, 1H), 7.68 (td, 1 H), 7.56 (dd, 1H), 7.47 (d, 1H), 7.39 (dd, 1H) Intermediate 252 1H NMR: (400 MHz, dmso-d6) δ ppm 9.84 (s, 1H), 8.59 (d, 1H), 7.69 (d, 1H), 7.5-7.3 (m, 5H) Intermediate 253 1H NMR: (400 MHz, dmso-d6) δ ppm 9.64 (s, 1H), 8.04 (dd, 1H), 7.62 (d, 1H), 7.5 (m, 1H), 7.5 (m, 3 H), 7.32 (dd, 1H) Intermediate 254 1H NMR: (400 MHz, dmso-d6) δ ppm 9.8 (s, 1H), 8 (dd, 1H), 7.45 (m, 3H), 7.15 (m, 2H), 7.1 (dd, 1 H), 5.25 (sec, 2H), 3.4 (sec, 3H) Intermediate 255 NMR Ή: (400 MHz, dmso-d6) δ ppm 10.75 (s, 1H), 9.95 (s, 1H), 7.85 (d, 1H), 7.75 (d, 1H), 7.25 (d, 1 H), 7.2 (d, 1H), 6.95 (dd, 1H), 6.9 (s, 1H) GC-EI (70eV^: [M]+. = 204 Intermediate 256 NMR Ή: (400 MHz, dmso-d6) δ ppm 10.6 (s, 1H), 9.7 (s, 1H), 7.8 (d, 1H), 7.05 (d, 1H), 7 (s, 1 H), 6.9 (m, 2H), 6.8 (s, 1H), 3.8 (2s, 6H) Intermediate 257 1 H NMR: (300 MHz, CDC13) δ ppm 9.9 (s, 1 H), 8.09 (dd, 1 H), 7.5 / 7.4 (bulk, 5 H), 7.21 (dd, 1 H), 7.15 (dd, 1H) NMR 19 F: (300 MHz, CDC13) δ ppm -103.7 Intermediate 258 1H NMR: (400 MHz, CDC13) δ ppm 10 (s, 1 H), 8.73 (d, 2 H), 8.08 (dd, 1 H), 7.71 (dt, 1 H), 7.61 (dt, 1 H) , 7.42 (dd, 1H), 7.35 (d, 2H) Intermediate 259 NMR Ή: (400 MHz, CDC13) δ ppm 10.1 (d, 1 H), 8 (dd, 1 H), 7.62 (dt, 1 H), 7.48 (2*m, 2 H), 7.46 (dd, 1 H), 7.3 (dd, 1H), 7.2 (dd, 1H) Intermediate 260 NMR Ή: (400 MHz, CDC13) δ ppm 9.99 (s, 1H), 8.71 (dd, 1H), 8.67 (d, 1H), 8.07 (dl, 1H), 7.75 (dt, 1H) , 7.7 (tl, 1H), 7.59 (tl, 1H), 7.44 (dd, 1H), 7.43 (dl, 1H) Intermediate 261 1H NMR: (300 MHz, CDC13) δ ppm 9.9 (d, 1H), 8.74 (dd, 1H), 8.69 (dd, 1H), 8.12 (dd, 1H), 7.74 (ddd, 1H) , 7.47 (dd, 1H), 7.28 (m, 1H), 7.15 (dd, 1H) NMR 19 F: (300 MHz, CDC13) δ ppm -102.6 Intermediate 262 1H NMR: (400 MHz, CDC13) δ ppm 9.89 (s, 1H), 8.75 (d, 2H), 8.11 (dd, 1H), 7.33 (d, 2H), 7.27 (td, 1H) , 7.12 (dd, 1H) Intermediate 263 1H NMR: (400 MHz, CDC13) δ ppm 9.82 (s, 1 H), 8.01 (d, 1 H), 7.45 (m, 3 H), 7.38 (m, 2 H), 6.94 (dd, 1 H) , 6.85 (df, 1H), 5.72 (si, 1H) Intermediate 264 1H NMR: (400 MHz, CDC13) δ ppm 9.68 (s, 1H), 9.35 (s, 1H), 8.5 (s, 1H), 8.15 (dd, 1H), 8.1 (m, 1H ), 7.75 (dt, 1H), 7.67 (2*m, 2H), 7.65 (dt, 1H), 7.51 (m, 1H), 7.47 (dd, 1H) GC-EI (70eV): [M]+. = 233.1 Intermediate 265 NMR Ή: (300 MHz, CDC13) δ ppm 9.9 (si, 1H), 8.03 (dd, 1H), 7.24 (d, 2H), 7.12 (td, 1H), 7.1 (dd, 1H) , 6.95 (d, 2H), 5.3 (s, 1H) NMR 19 F: (300 MHz, CDC13) δ ppm -102.4 Intermediate 266 NMR Ή: (400 MHz, dmso-d6) δ ppm 10.65 (s, 1H), 9.65 (s, 1H), 7.8 (d, 1H), 7.3 (s, 4H), 6.9 (dd, 1 H), 6.75 (s, 1H), 2.35 (d, 3H) Intermediate 267 NMR Ή: (400 MHz, dmso-d6) δ ppm 9.8 (s, 1H), 8.2 (d, 1H), 8.05 (d, 1H), 7.75 ( 7.7 (d, 1H), 7.35 (t , 1H), 7.25 (dd, 1H), 7.2 (s, 1H), 6.95 (t, 1H), 3.9 (s, 3H) Intermediate 268 1H NMR: (400 MHz, dmso-d6) δ ppm 9.75 (s, 1H), 8.69 (d, 2H), 7.97 (d, 1H), 7.7 (dd, 1H), 7.5 (d, 2 H), 7 (d, 1H), 3.9 (s, 3H) Intermediate 269 1H NMR: (300 / 400 MHz, dmso-d6) δ ppm 9.8 (s, 1H), 8 (dd, 1H), 7.55 (m, 1H), 7.5 (m, 1H), 7.45 (d , 1H), 7.45 (d, 1H), 7.35 (m, 1H), 7.3 (dd, 1H) NMR 19 F: (300 / 400 MHz, dmso-d6) δ ppm -103.1 , -1 1 1.7 Intermediate 270 1H NMR: (400 MHz, dmso-d6) δ ppm 10.75 (si, 1H), 9.65 (s, 1H), 7.81 (d, 1H), 7.45 (dd, 2H), 7.3 (dd, 2 H), 6.93 (dd, 1H), 6.75 (d, 1H) Intermediate 271 1H NMR: (400 MHz, CDC13) δ ppm 9.88 (s, 1H), 8.06 (dd, 1H), 7.36 (dd, 2H), 7.19 (m, 1H), 7.19 (dd, 2H) , 7.1 1 (dd, 1H) Intermediate 272 1H NMR: (400 MHz, CDC13) δ ppm 9.9 (s, 1H), 8.05 (dd, 1H), 7.28 (dd, 4H), 7.16 (td, 1H), 7.12 (dd, 1H ), 2.44 (s, 3H) Intermediate 273 1H NMR: (400 MHz, dmso-d6) δ ppm 9.82 (s, 1H), 8 (dd, 1H), 7.48-7.3 (m, 2H), 7.48-7.3 (m, 2H), 7 (ddd, 1H), 3.9 (s, 3H) NMR 19 F: (400 MHz, dmso-d6) δ ppm -104.4, -135.7 Intermediate 274 NMR Ή: (400 MHz, dmso-d6) δ ppm 9.8 (s, 1H), 8.05 (dd, 1H), 7.45 (m, 1H), 7.4 (d, 1H), 6.9 (s, 1 H), 3.45 (sec, 3H), 2.35 (sec, 3H) NMRUF: (400 MHz, dmso-d6) δ ppm -102.9 Intermediate 275 1H NMR: (400 MHz, dmso-d6) δ ppm 9.7 (s, 1H), 7.95 (d, 1H), 7.15 (dd, 1H), 7 (s, 1H), 6.85 (s, 1 H), 3.9 (s, 3H), 3.4 (s, 3H), 2.35 (s, 3H) Intermediate 276 NMR Ή: (300 / 400 MHz, dmso-d6) δ ppm 9.7 (s, 1H), 7.93 (d, 1H), 7.8 (s, 1H), 7.18 (dd, 1H), 7.03 (d , 1H), 7 (s, 1H), 3.9 (s, 3H), 3.54 (s, 3H) Intermediate 277 1H NMR: (400 MHz, CDC13) δ ppm 9.85 (s, 1H), 8.15 (dd, 1H), 7.6 (s, 1H), 7.3 (m, 1H), 7.15 (d, 1H) , 6.35 (s, 1H), 3.75 (s, 3H) NMR 19 F: (400 MHz, CDC13) δ ppm -101.2 Intermediate 278 1H NMR: (400 MHz, dmso-d6) δ ppm 9.9 (s, 1H), 7.98 (dd, 1H), 7.9 (d, 1H), 7.84 (d, 1H), 7.78 (td, 1 H), 7.77 (dd, 1H), 7.67 (tl, 1H), 7.55 (dd, 1H) IED (70eV): [M]+. = 284 Intermediate 279 1H NMR: (400 MHz, dmso-d6) δ ppm 9.9 (s, 1H), 7.9 (d, 1H), 7.75 (m, 1H), 7.55 (m, 1H), 7.5 (d, 1 H), 7.1 (s, 1H), 7.05 (d, 1H), 6.85 (dd, 1H), 6.1 (s, 2H) Intermediate 280 NMR Ή: (400 MHz, dmso-d6) δ ppm 9.8 (s, 1H), 7.99 (d, 1H), 7.8 (t, 1H), 7.69 (t, 1H), 7.58 (d, 1 H), 7.55 (d, 1H), 6.41 (d, 1H), 3.69 (s, 3H) NMR 13 C: (400 MHz, dmso-d6) δ ppm 191, 138, 138, 136, 134, 133, 132, 130, 128, 109, 37 Intermediate 281 1H NMR: (400 MHz, dmso-d6) δ ppm 9.9 (s, 1H), 7.91 (d, 1H), 7.75 (t, 1H), 7.59 (t, 1H), 7.54 (d, 1 H), 7.42 (t, 1H), 7.05 (dd, 1H), 7.01 (t, 1H), 6.98 (dd, 1H), 3.82 (s, 3H) Intermediate 282 1H NMR: (400 MHz, dmso-d6) δ ppm 9.66 (s, 1H), 7.86 (d, 1H), 7.73 (t, 1H), 7.54 (t, 1H), 7.46 (t, 1 H), 7.38 (d, 1H), 7.31 (d, 1H), 7.14 (d, 1H), 7.1 1 (t, 1H), 3.69 (s, 3H) Intermediate 283 Ή NMR: (400 MHz, dmso-d6) δ ppm 9.86 (s, 1H), 8.17 (d, 1H), 7.78 (d, 1H), 7.7-7.55 (m, 1H), 7.7-7.55 (m, 5H), 7.52 (t, 1H) Intermediate 284 1H NMR: (400 MHz, dmso-d6) δ ppm 9.82 (d, 1H), 8.17 (dd, 1H), 7.62 (d, 2H), 7.52 (m, 3H), 7.43 (d, 1 H) Intermediate 285 1H NMR: (400 MHz, CDC13) δ ppm 9.85 (s, 1 H), 8.03 (d, 1 H), 7.5-7.37 (m, 5 H), 7 (dd, 1 H), 6.89 (df, 1 H), 3.9 (sec, 3H) Intermediate 286 RM Ή: (400 MHz, dmso-d6) δ ppm 9.89 (s, 1H), 7.95 (d, 1H), 7.77 (t, 1H), 7.62 (m, 3 H), 7.53 (d, 1H), 7.49 (d, 2H) NMR 19F: (400 MHz, dmso-d6) δ ppm -55.59 Intermediate 287 1H NMR: (400 MHz, CDC13) δ ppm 9.9 (d, 1H), 8.04 (dd, 1H), 7.68 (dt, 1H), 7.56 (t, 1H), 7.39 (d, 1H) , 7.31 (dt, 1H), 7.01 (dt, 1H), 6.95 (dt, 1H) NMR 19 F: (400 MHz, CDC13) δ ppm - 109 / - 110 Intermediate 288 NMR Ή: (400 MHz, CDC13) δ ppm 10 (d, 1 H), 8.01 (dd, 1 H), 7.63 (dt, 1 H), 7.48 (t, 1 H), 7.44 (d, 1 H) , 7.29 (s, 4H), 2.43 (s, 3H) Intermediate 289 NMR Ή: (400 MHz, CDC13) δ ppm 10 (s, 1 H), 8.02 (d, 1 H), 7.62 (t, 1 H), 7.45 (d, 1 H), 7.32 (2*d, 4 H), 4.48 (t, 1H), 2.99 (hept., 1H), 1.31 (d, 6H) Intermediate 290 1H NMR: (400 MHz, CDC13) δ ppm 10.27 (d, 1 H), 7.99 (dd, 1 H), 7.61 (dt, 1 H), 7.55 (2*m, 2 H), 7.46 (2*m , 2H), 6.59 (dd, 1H) Intermediate 291 1H NMR: (300 MHz, dmso-d6) δ ppm 9.99 (s, 1H), 8.86 (d, 1H), 8.82 (df, 1H), 7.79 (dd, 1H), 7.6 (2*d , 4H) Intermediate 292 1H NMR: (400 MHz, dmso-d6) δ ppm 9.85 (s, 1H), 7.95 (d, 1H), 7.65 (dd, 1H), 7.6 (s, 1H), 7.55 (d, 2 H), 7.5 (d, 2H) Intermediate 293 1H NMR: (400 MHz, dmso-d6) δ ppm 9.7 (s, 1H), 8 (dd, 1H), 7.8 (td, 1H), 7.7 (td, 1H), 7.65 (d, 1 H), 7.55 (dd, 1H), 6.5 (d, 1H), 5 (dd, 1H), 3.8 / 3.25 (2m, 2H), 2.25 / 1.8 (2m, 2H), 1.9 / 1.5 (2m, 2H), 1.4 (m, 2H) Procedure F: Generic procedure for reductive amination from intermediate 21 (synthesis of intermediates 22 to 127). Intermediate 21 (14 g, 26.2 mmol) of anhydrous DCM (280 mL), aldehyde (intermediates 213 to 293) (39.3 mmol, 1.5 eq) as well as MgSC 3 (14 g). After lh of agitation, NaBH(OAc) 3 (8.32 g, 39.3 mmol, 1.5 eq) is added in portions and the reaction mixture is maintained at ambient temperature for 16 h. The reaction is monitored by LC / MS. The insolubles are filtered through microfibre and rinsed with DCM (100 mL). The filtrate is then washed with water (1 x 200 mL) then with a saturated NaCl solution (2 x 200 mL). The organic phase is dried over MgSC 4 and concentrated under reduced pressure. The oil obtained is then purified by flash chromatography on silica gel (330g) to lead to intermediates 22 to 127. EXAMPLE 31: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 31 is obtained from intermediate 21 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 3.5-3.65 (2m, 2H), 3.2 (m, 1H), 3.05 (dd, 1H), 2.95 (m, 2H), 2.15 (m, 1 H), 1.95 (m, 1H), 1.75 (m, 1H), 1.65 (m, 2H), 1.5 (m, 1H), 1.4 (m, 1H), 1.25 (m, 1H) ESI / FIA / HR and MS / MS: [M+H]+ = 251.1154 (251.1160) Elemental Analysis: C=42.65(43.20);H=7.23(7.65);N=11.24(11.20) Intermediate 22: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[(3-fluoro-4-hydroxyphenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane- Tert-butyl 3-carboxylate Intermediate 22 is obtained from intermediate 21 and 3-fluoro-4-hydroxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.0 (d, 1H), 6.88 (d, 2H), 3.95 (m, 2H), 3.5 / 3.33 (2*d, 2H), 3.4 (m, 2H), 2.85 / 2.3 (2*m, 2H), 2.8 / 2.45 (dd, 2H), 2-1.6 (m, 4H), 1.42 / 1.35 (2*s, 27H) , 1.4 (m, 2H), 1.2 (t, 3H), 0.9 (m, 2H) EXAMPLE 32: 3-(4-Aminobutyl)-1-[(3-fluoro-4-hydroxyphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 32 is obtained from intermediate 22 according to procedure D previously described. 1H NMR: (300 / 400 MHz, D20) δ ppm 7.24 (dd, 1H), 7.12 (dd, 1H), 7.03 (t, 1H), 4.32 / 4.12 (2*d, 2H), 3.68 / 3.3 (2*m, 2H), 3.45 / 3.07 (2*m, 2H), 2.92 (m, 2H), 2.22 / 1.78 (2*m, 2H), 1.92 / 1.58 (2*m , 2H), 1.58 / 1.46 (2*m, 2H), 1.23 / 1.1 (2*m, 2H) NMR 19 F: (300 / 400 MHz, D20) δ ppm -135.8 ESI / FIA / HR and MS / MS: [M+H]+ = 375.1455 (375.1480) Elemental Analysis: C=51.71(51.34);H=6.44(6.46);N=7.64(7.48) Intermediate 23: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[(2,4-difluorophenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate tert-butyl Intermediate 23 is obtained from intermediate 21 and 2,4-difluorobenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.44 (m, 1H), 7.19 (m, 1H), 7.07 (m, 1H), 4 (m, 2H), 3.57 (m, 2 H), 3-2.6 / 2.35 (m, 2H), 3-2.6 / 2.52 (m, 2H), 2.78 (m, 2H), 2-1.6 (m, 2H), 2- 1.6 (m , 2H), 1.39 (m, 27H), 1.39 (m, 2H), 1.2 (m, 3H), 0.82 (m, 2H) EXAMPLE 33: 3-(4-Aminobutyl)-1-[(2,4-difluorophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 33 is obtained from of intermediate 23 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.51 (m, 1H), 7.07 (m, 2H), 4.37 (si, 2H), 3.69 / 3.33 (m, 2H), 3.49 / 3.19 (m , 2H), 2.95 (m, 2H), 2.21 / 1.77 (m, 2H), 1.95 / 1.49 (m, 2H), 1.61 (m, 2H), 1.28 / 1.14 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 377.1419 (377.1441) Elemental Analysis: C=50.66(51.06);H=5.79(6.16);N=7.37(7.44) Intermediate 24: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[(3,5-difluoro-4-hydroxyphenyl)methyl]-4-ethoxy-4-oxo-1,4- tert-butyl azaphosphinane-3-carboxylate Intermediate 24 is obtained from intermediate 21 and 3,5-difluoro-4hydroxy-benzaldehyde according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 10.1 (si, 1H), 6.63 (d, 2H), 4.1-3.8 (m, 2H), 3.58-3.3 (m, 2H), 3.58 -3.3 (m, 2 hrs), 3-2.6 / 2.3 (2*m, 2 hrs), 3-2.6 / 2.49 (2*m, 2 hrs), 2-1.5 (m, 2 hrs), 2-1.5 (m, 2H), 1.4 (m, 2H), 1.4 / 1.37 (2*s, 27H), 1.2 (t, 3H), 1.1-0.8 (m, 2H) EXAMPLE 34: 3-(4-Aminobutyl)-1-[(3,5-difluoro-4-hydroxyphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 34 is obtained from intermediate 24 according to procedure D previously described. 1H NMR: (300 / 400 MHz, D20) δ ppm 7.1 (m, 2 H), 4.33 / 4.12 (2*d, 2 H), 3.69 / 3.31 (2*dd, 2 H), 3.45 / 3.09 (2*dd, 2H), 2.94 (m, 2H), 2.24 / 1.78 (2*m, 2H), 1.93 / 1.6 (2*m, 2H), 1.6 / 1.47 (2*m, 2H), 1.25 / 1.13 (2*m, 2H) NMR 19 F: (300 / 400 MHz, D20) δ ppm -132 ESI / FIA / HR and MS / MS: [M+H]+ = 393.1388 (393.1390) Elemental Analysis: C=48.74(48.98);H=5.90(5.91);N=7.10(7.14) Intermediate 25: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[[4- tert-Butyl (difluoromethyl)phenyl]methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 25 is obtained from intermediate 21 and 4-(difluoromethyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.55-7.4 (dd, 4H), 7 (t, 1H), 4.1-3.85 (m, 2H), 3.7- 3.5 (dd, 2H) , 3.35 (m, 2 hrs), 3-2.25 (m, 4 hrs), 2-1.8 (m, 4 hrs), 1.4 (m, 2 hrs), 1.4 (s, 18 hrs), 1.35 (s, 9 H), 1.2 (t, 3H), 0.8 (m, 2H). EXAMPLE 35: 3-(4-Aminobutyl)-1-[[4-(difluoromethyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 35 is obtained from intermediate 25 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.7-7.6 (d, 4H), 6.85 (t, 1H), 4.5 / 4.3 (m, 2H), 3.8-3.65 (m, 1H), 3.55 -3.35 (m, 2H), 3.15 (m, 1H), 2.95 (m, 2H), 2.25 (m, 1H), 2-1.75 (m, 2H), 1.65-1.5 (m, 3 H), 1.3-1.1 (m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 26 NMR 19 F: (400 MHz, D20) δ ppm -110 ESI / FIA / HR and MS / MS: [M+H]+ = 391.1583 (391.1598) Elemental Analysis: C=51.85(52.31);H=6.46(6.45);N=7.04(7.18) Intermediate 26: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-hydroxy-3-(trifluoromethyl)phenyl]methyl]-4-oxo-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 26 is obtained from intermediate 21 and 4-hydroxy-3-(trifluoromethyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 10.45 (massive, 1H), 7.4 (si, 1H), 7.34 (dl, 1H), 6.96 (d, 1H), 4.1-3.85 (m , 2H), 3.65-3.3 (m, 2H), 3.65-3.3 (m, 2H), 3-2.2 (m, 4H), 2-1.6 (m, 4H), 1.38 (m, 29 H), 1.2 (t, 3 H), 0.88 (m, 2 H) EXAMPLE 36: Acid 3-(4-aminobutyl)-4-hydroxy-1-[[4-hydroxy-3- (trifluor omethyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 36 is obtained from intermediate 26 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.68 (df, 1 H), 7.55 (dd, 1 H), 7.09 (d, 1 H), 4.38 / 4.2 (2*d, 2 H), 3.7 / 3.3 (2*dd, 2H), 3.45 / 3.09 (2*dd, 2H), 2.92 (m, 2H), 2.23 / 1.77 (2*m, 2H), 1.93 / 1.6 (2*m, 2 H), 1.6 / 1.47 (2*m, 2H), 1.25 / 1.11 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 425.1453 (425.1453) Elemental Analysis C=48.19(48.12);H=5.16(5.70);N=6.72(6.60) Intermediate 27: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-1-[(3-chloro-5-fluoro-4-hydroxyphenyl)methyl]-4-ethoxy-4-oxo- Tert-butyl 1,4-azaphosphinane-3-carboxylate Intermediate 27 is obtained from intermediate 21 and 3-chloro-5-fluoro-4-hydroxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 10.26 (si, 1H), 7.12 (si, 1H), 7.07 (dl, 1H), 4.06 / 3.98 (2quad, 2H), 3.47 (AB , 2H), 3.42 (m, 2H), 3-2.26 (m, 4H), 1.94 (m, 4H), 1.41 / 1.37 (2s, 27H), 1.4 (m, 2H), 1.25 / 1.21 (2t, 3H), 0.92 (m, 2H) NMR 19 F: (400 MHz, dmso-d6 δ ppm -131.7 NMR 31 P: (400 MHz, dmso-d6) δ ppm -43 ESI / FIA / HR and MS / MS: [M+H]+ = 693.308 (693.3083) EXAMPLE 37: 3-(4-Aminobutyl)-1-[(3-chloro-5-fluoro-4-hydroxyphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 37 is obtained from intermediate 27 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.3 (m, 1 H), 7.21 (m, 1 H), 4.31 / 4.12 (2*d, 2 H), 3.69 / 3.3 (2*dd, 2 H) , 3.45 / 3.09 (2*dd, 2H), 2.93 (m, 2H), 2.24 / 1.77 (2*m, 2H), 1.93 / 1.6 (2*m, 2H), 1.6 / 1.47 (2 *m, 2H), 1.27 / 1.13 (2*m, 2H) NMR 19 F: (400 MHz, D20) δ ppm -131.6 ESI / FIA / HR and MS / MS: [M+H]+ = 409.1091 (409.1095) Elemental Analysis: C=47.25(47.01);H=5.75(5.67);N=6.92(6.85) Intermediate 28: 3-{4-[Bis(teri-butoxycarbonyl)amino]butyl}-1-(2,3-dihydro-1-benzofuran-5-ylmethyl)-4-ethoxy-4-oxo-1,4- tert-butyl azaphosphinane-3-carboxylate Intermediate 28 is obtained from intermediate 21 and 2,3-dihydrobenzofuran-5-carbaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.13 (d, 1H), 6.97 (dd, 1H), 6.68 (d, 1H), 4.5 (t, 2H), 4 (m, 2 H), 3.55-3.3 (m, 4H), 3.15 (m, 2H), 3-2.2 (m, 4H), 1.91 (m, 4H), 1.39 (m, 29H), 1.2 (t , 3H), 0.87 (m, 2H) EXAMPLE 38: 3-(4-Aminobutyl)-1-(2,3-dihydro-1-benzofuran-5-ylmethyl)-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 38 is obtained from intermediate 28 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.34 (d, 1 H), 7.2 (dd, 1 H), 6.85 (d, 1 H), 4.59 (t, 2 H), 4.14 / 3.68 (dd, 2 H), 3.68 / 3.28 (m, 2H), 3.47 / 3.06 (m, 2H), 3.22 (t, 2H), 2.94 (m, 2H), 2.22 / 1.76 (m, 2H), 1.93 / 1.47 (m, 2H), 1.6 (m, 2H), 1.26 / 1.12 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 383.1725 (383.1735) Elemental Analysis: C=55.92(56.54);H=6.71(7.12);N=7.17(7.33) Intermediate 29: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-OXO-3H-1,3-benzoxazol-6-yl) methyl]-tert-butyl 1,4-azaphosphinane-3-carboxylate Intermediate 29 is obtained from intermediate 21 and 3H-1,3-benzoxazolecarbaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 12.55 (s, 1H), 7.15 (s, 1H), 7.05 (dd, 1H), 7 (d, 1H), 4 (m, 2 H), 3.65 (d, 1H), 3.4 (d, 1H), 3.35 (m, 2H), 3.05-2.3 (m, 4H), 2.05-1.8 (m, 4H), 1.4 (m , 2H), 1.4 (3s, 27H), 1.25 (t, 3H), 0.9-0.7 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 682.3461 (682.3468) EXAMPLE 39: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-oxo-3H-1,3-benzoxazol-6-yl)methyl]-1,4-azaphosphinan-3-acid -carboxylic Example 39 is obtained from intermediate 29 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.4 (s, 1H), 7.3 (dd, 1H), 7.25 (d, 1H), 4.45 / 4.25 (2dd, 2H), 3.8-3.6 (m , 1H), 3.45 (m, 1H), 3.35 (m, 1H), 3.1 (m, 1H), 2.95 (m, 2H), 2.25 (m, 2H), 1.95 (m, 1 H), 1.65-1.4 (m, 3H), 1.25 / 1.1 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 398.1455 (398.1480) Elemental Analysis: C=51.17(51.39);H=5.85(6.09);N=10.49(10.57) Intermediate 30: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-(1H-benzimidazol-5-ylmethyl)-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate tert-butyl Intermediate 30 is obtained from intermediate 21 and 1H-benzimidazole-5-carbaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 12.4 (si, 1H), 8.16 (s, 1H), 7.7-7.3 (m, 2H), 7.14 (d, 1H), 3.97 (m , 2H), 3.72 / 3.54 (2*d, 2H), 3.45-3.2 (m, 2H), 2.97 / 2.33 (2*m, 2H), 2.85 / 2.48 (2*m, 2H) , 2.02-1.85 (m, 2H), 2.02-1.85 (m, 2H), 1.39 / 1.34 (2*s, 27H), 1.38 (m, 2H), 1.2 (t, 3H), 0.81 (m, 2H) EXAMPLE 40: 3-(4-Aminobutyl)-1-(1H-benzimidazol-5-ylmethyl)-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 40 is obtained from the intermediate 30 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.26 (s, 1 H), 7.77 (df, 1 H), 7.72 (d, 1 H), 7.38 (dd, 1 H), 4.53 / 4.34 (2*d , 2H), 3.73 / 3.36 (2*m, 2H), 3.47 / 3.12 (2*m, 2H), 2.88 (m, 2H), 2.23 / 1.78 (2*m, 2H), 1.91 / 1.55 ​​(2*m, 2H), 1.55 / 1.45 (2*m, 2H), 1.18 / 1.04 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 381.1692 (381.1691) Elemental Analysis: C=54.46(53.68);H=6.00(6.62);N=14.67(14.73) Intermediate 31: 3-{4-[Bis(tert-butoxycarbonyl)amino]butyl}-1-[(2-fluoro-4-hydroxyphenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane- Tert-butyl 3-carboxylate Intermediate 31 is obtained from intermediate 21 and 2-fluoro-4-methoxy-benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.25 (t, 1H), 6.78 (2*m, 2H), 4.1-3.9 (m, 2H), 3.76 (s, 3H), 3.57 / 3.46 (2*d, 2H), 3.36 (m, 2H), 2.93 / 2.32 (2*m, 2H), 2.81 / 2.47 (2*dd, 2H), 2- 1.8 (m, 2 H), 2-1.8 (m, 2H), 1.42 / 1.36 (2*s, 27H), 1.4 (m, 2H), 1.2 (t, 3H), 1-0.75 (m, 2H) EXAMPLE 41: 3-(4-Aminobutyl)-1-[(2-fluoro-4-hydroxyphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 41 is obtained from intermediate 31 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.21 (t, 1 H), 6.63 (m, 1 H), 6.63 (m, 1 H), 4.19 (dd, 2 H), 3.58 / 3.19 (m, 2 H), 3.38 / 3.04 (dd, 2H), 2.84 (m, 2H), 2.1 / 1.65 (m, 2H), 1.84 / 1.5 (m, 2H), 1.5 / 1.38 (m, 2H) , 1.17 / 1.04 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 375.1486 (375.1485) Elemental Analysis: C=51.05(51.34);H=5.28(6.46);N=7.76(7.48) Intermediate 32: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4 tert-Butyl -oxo-1-[(6-oxo-1H-pyridin-3-yl)methyl]-1,4-azaphosphinane-3-carboxylate Intermediate 32 is obtained from intermediate 21 and 6-hydroxynicotinaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 11.45 (s, 1H), 7.35 (dd, 1H), 7.21 (df, 1H), 6.31 (d, 1H), 4.1-3.9 (m , 2H), 3.4 (m, 2H), 3.32 / 3.19 (2*d, 2H), 2.9 / 2.28 (2*m, 2H), 2.8 / 2.44 (2*dd, 2H), 2 -1.7 (m, 2H), 2-1.7 (m, 2H), 1.42 / 1.38 (2*s, 27H), 1.4 (m, 2H), 1.21 (t, 3H), 1.1- 0.85 (m, 2H) EXAMPLE 42: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(6-oxo-1H-pyridin-3-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 42 is obtained from intermediate 32 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.74 (dd, 1 H), 7.7 (d, 1 H), 6.66 (d, 1 H), 4.17 (AB, 2 H), 3.69 / 3.31 (2m, 2 H), 3.45 / 3.09 (2m, 2H), 2.94 (m, 2H), 2.24 / 1.79 (2m, 2H), 1.94 / 1.49 (2m, 2H), 1.61 (quint., 2H), 1.29 / 1.14 (2m, 2H) NMR 31 P: (300 MHz, D20) δ ppm 25.8 ESI / FIA / HR and MS / MS: [M+H]+ = 358.1537 (358.1531) Elemental Analysis: C=50.77(50.42);H=6.41(6.77);N=11.96(11.76) Intermediate 33: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-(1-benzofuran-5-ylmethyl)-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate tert-butyl Intermediate 33 is obtained from intermediate 21 and 5-formylbenzofuran according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.98 (df, 1H), 7.55 (df, 1H), 7.53 (d, 1H), 7.25 (dd, 1H), 6.91 (df, 1 H), 4.1-3.9 (m, 2H), 3.72 / 3.51 (2*d, 2H), 3.4-3.2 (m, 2H), 2.98 / 2.35 (2*dd, 2H), 2.81 / 2.48 (2*dd, 2H), 2-1.65 (m, 2H), 2-1.65 (m, 2H), 1.4 / 1.34 (2*s, 27H), 1.39 (m, 2H), 1.21 (t, 3 H), 1-0.7 (m, 2 H) EXAMPLE 43: 3-(4-Aminobutyl)-1-(1-benzofuran-5-ylmethyl)-4-hydroxy-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 43 is obtained from intermediate 33 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.79 (df, 1 H), 7.76 (df, 1 H), 7.61 (d, 1 H), 7.39 (dd, 1 H), 7.31 / 4.5 (2*d , 2H), 6.91 (df, 1H), 3.72 / 3.33 (2*dd, 2H), 3.49 / 3.11 (2*dd, 2H), 2.9 (m, 2H), 2.23 / 1.77 (2 *m, 2H), 1.91 / 1.57 (2*m, 2H), 1.57 / 1.45 (2*m, 2H), 1.2 / 1.15 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 381.1577 (381.1579) Elemental Analysis: C=56.67(56.84);H=6.52(6.62);N=7.42(7.36) Intermediate 34: 3-{4-[Bis(tert-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-hydroxy-2-methylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3 tert-butyl-carboxylate Intermediate 34 is obtained from intermediate 21 and 4-methoxy-2-methylbenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.05 (d, 1H), 6.75 (df, 1H), 6.69 (dd, 1H), 4.1-3.9 (m, 2H), 3.72 (s , 3H), 3.5 / 3.3 (2*d, 2H), 3.3 (m, 2H), 2.9 / 2.41 (2*m, 2H), 2.8 / 2.29 (2*m, 2H), 2.3 (2*s, 3H), 2.02-1.79 (massive, 2H), 2.02-1.79 (massive, 2H), 1.42 / 1.36 (2*s, 27H), 1.32 (m, 2H), 1.21 (t, 3H), 0.68 (m, 2H) EXAMPLE 44: 3-(4-Aminobutyl)-4-hydroxy-1-[(4-hydroxy-2-methylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 44 is obtained from intermediate 34 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.25 (d, 1 H), 6.81 (df, 1 H), 6.77 (dd, 1 H), 4.29 / 4.22 (2*d, 2 H), 3.69 / 3.32 (2*dd, 2H), 3.49 / 3.18 (2*dd, 2H), 2.94 (m, 2H), 2.32 (s, 3H), 2.19 / 1.75 (2*m, 2H), 1.94 / 1.6 (2*m, 2H), 1.6 / 1.5 (2*m, 2H), 1.27 / 1.12 (2*m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 26 ESI / FIA / HR and MS / MS: [M+H]+ = 371.1739 (371.1735) Elemental Analysis: C=54.81(55.13);H=6.88(7.35);N=7.52(7.56) Intermediate 35: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[(2-chloro-4-fluorophenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3 - tert-butyl carboxylate Intermediate 35 is obtained from intermediate 21 and 2-chloro-4-fluorobenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.5 (dd, 1H), 7.35 (dd, 1H), 7.2 (dd, 1H), 4.1-3.9 (quad., 2H), 3.65- 3.55 (d, 2H), 3.4-3.3 (m, 2H), 2.9-2.35 (m, 4H), 1.9 (m, 4H), 1.55-1.35 (m, 2H), 1.4-1.35 ( s, 27H), 1.2 (t, 3H), 0.85-0.75 (m, 2H) NMR 31 P: (400 MHz, dmso-d6) δ ppm 45 NMR 19 F: (400 MHz, dmso-d6) δ ppm -112 ESI / FIA / HR and MS / MS: [M+H]+ = 677.3146 (677.3133) EXAMPLE 45: 3-(4-Aminobutyl)-1-[(2-chloro-4-fluorophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 45 is obtained from intermediate 35 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.56 (dd, 1 H), 7.39 (dd, 1 H), 7.18 (td, 1 H), 4.43 (si, 2 H), 3.7 / 3.4 (m, 2 H), 3.5 / 3.26 (m, 2H), 2.95 (m, 2H), 2.22 / 1.78 (m, 2H), 1.95 / 1.62 (m, 2H), 1.62 / 1.5 (m, 2H) , 1.28 / 1.12 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 393.1149 (393.1146) Elemental Analysis C=49.40(48.93);H=5.31(5.90);N=7.17(7.13) Intermediate 36: 3-{4-[Bis(ter^butoxycarbonyl)amino]butyl}-1-[[2-(4-fluorophenyl)phenyl]methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane- Tert-butyl 3-carboxylate Intermediate 36 is obtained from intermediate 21 and 2-(4-fluorophenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.5-7.2 (m, 4H), 7.5-7.2 (m, 4H), 4.08-3.73 (m, 2H), 3.52 / 3.3 (2*d , 2H), 3.3 (m, 2H), 2.8-2.62 / 2.33 (2*m, 2H), 2.8-2.62 / 2.2 (2*m, 2H), 1.98- 1.63 (m, 2H) , 1.98-1.63 (m, 2H), 1.4 / 1.32 (2*s, 27H), 1.38 (m, 2H), 1.21 / 1.18 (2*t, 3H), 0.9-0.6 (m, 2 h) EXAMPLE 46: 3-(4-Aminobutyl)-1-[[2-(4-fluorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 46 is obtained from intermediate 36 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.6 (d, 1H), 7.52 (m, 2H), 7.4 (d, 1H), 7.35 (dd, 2H), 7.24 (dd, 2H) , 4.41 / 4.29 (dd, 2H), 3.39 / 3.1 (2*m, 2H), 3.19 / 2.88 (2*m, 2H), 2.93 (m, 2H), 2.09 / 1.65 (2*m , 2H), 1.85 / 1.59 (2*m, 2H), 1.59 / 1.35 (2*m, 2H), 1.2-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 435.1850 (435.1848) Elemental Analysis: C=60.73(60.82);H=5.96(6.50);N=6.73(6.45) Intermediate 37: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[[2-( tert-Butyl 2-fluorophenyl)phenyl]methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 37 is obtained from intermediate 21 and 2-(2-fluorophenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.52 (d, 1H), 7.45 / 7.42 (t, 2H), 7.45 (m, 1H), 7.35 (m, 3H), 7.2 (d , 1H), 3.91 (m, 2H), 3.5-3.2 (m, 2H), 3.5-3.2 (m, 2H), 2.67 / 2.29 (m, 2H), 2.67 / 2.13 (m, 2 H), 1.95-1.6 (m, 2H), 1.95-1.6 (m, 2H), 1.42 (s, 18H), 1.38 (m, 2H), 1.34 (s, 9H), 1.17 (t , 3H), 0.68 (m, 2H) EXAMPLE 47: 3-(4-Aminobutyl)-1-[[2-(2-fluorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 47 is obtained from intermediate 37 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.66 (m, 1H), 7.57 (m, 1H), 7.57 (m, 1H), 7.51 (m, 1H), 7.42 (m, 1H) , 7.34 (m, 1H), 7.34 (m, 1H), 7.28 (t, 1H), 4.6-4 (massive, 2H), 3.7-2.7 (massive, 2H), 3.7-2.7 (massive , 2H), 2.93 (m, 2H), 2.14 / 1.69 (m, 2H), 1.87 / 1.37 (m, 2H), 1.59 (m, 2H), 1.15 / 1.06 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 435.1855 (435.1848) Elemental Analysis: C=60.87(60.82);H=6.12(6.50);N=6.42(6.45) Intermediate 38: 3-{4-[Bis(ter^butoxycarbonyl)amino]butyl}-1-[[2-(2,5-dichlorophenyl)phenyl]methyl]-4-ethoxy-4-oxo-1,4- tert-butyl azaphosphinane-3-carboxylate Intermediate 38 is obtained from intermediate 21 and 2-(2,5-dichlorophenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.65-7.1 (m, 7H), 4.05-3.85 (m, 2H), 3.5-3.2 (m, 4H), 2.8-2.3 (m, 4 H), 2.2-1.65 (m, 4H), 1.5-1.3 (m, 2H), 1.45 (s, 18H), 1.35 (s, 9H), 1.2 (t, 3H), 0.8-0.5 (m, 2H) EXAMPLE 48: 3-(4-Aminobutyl)-1-[[2-(2,5-dichlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 48 is obtained from intermediate 38 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.7-7.3 (m, 7 H), 4.45 / 4.21 / 4.02 (m, 2 H), 3.75 / 3.1 (2*m, 2 H), 3.75 / 3.1 (2 *m, 2H), 2.98 (m, 2H), 2.2 / 1.65 (2*m, 2H), 1.95 / 1.65 (2*m, 2H), 1.65 / 1.15 (2*m, 2H) , 1.45 / 1.15 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 485.1184 (485.1163) Elemental Analysis: C=54.33(54.44);H=4.99(5.61);N=5.86(5.77) Intermediate 39: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[[2-(3-phenylphenyl)phenyl]methyl]-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 39 is obtained from intermediates 21 and 241 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.7 (d, 2 H), 7.65 (d, 1 H), 7.6 (s, 1 H), 7.55 (m, 2 H), 7.45 (m, 2 H), 7.4-7.3 (m, 5H), 3.9 (m, 2H), 3.6 / 3.4 (2*d, 2H), 3.4-3.2 (m, 2H), 2.85-2.65 (m, 2 H), 2.35 (m, 1H), 2.2 (m, 1H), 1.9 (m, 1H), 1.85-1.6 (m, 3H), 1.45-1.3 (m, 2H), 1.4 / 1.3 (2*s, 27 H), 1.15 (t, 3 H), 0.65 (m, 2 H) EXAMPLE 49: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[2- (3-phenylphenyl)phenyl]methyl]-l,4-azaphosphinane-3-carboxylic acid Example 49 is obtained from intermediate 39 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.6-7.1 (m, 13 H), 4.25 (d, 1 H), 4.1 (d, 1 H), 3.4-3.2 (m, 1 H), 3.15-2.9 (m, 2H), 2.75-2.55 (m, 3H), 2.05 (m, 1H), 1.75 (m, 1H), 1.55 (m, 1H), 1.4 (m, 2H), 1.25 (m, 1H), 0.9 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 493.2256 (493.2256) Elemental Analysis: C=68.08(68.28);H=6.02(6.75);N=5.71(5.69) Intermediate 40: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(2-naphthalen-2-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane -3- tert-butyl carboxylate Intermediate 40 is obtained from intermediates 21 and 240 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.95 (d, 1H), 7.95 (m, 2H), 7.9 (s, 1H), 7.55 (m, 4H), 7.4 (m, 2 H), 7.3 (d, 1H), 3.9 (m, 2H), 3.65 / 3.45 (2*d, 2H), 3.45-3.2 (m, 2H), 3.3-2.6 (m, 2H) , 2.35 (dd, 1H), 2.2 (m, 1H), 1.9 (m, 1H), 1.85-1.65 (m, 3H), 1.8 (m, 2H), 1.4 / 1.3 (2*s , 27H), 1.15 (t, 3H), 0.7 (m, 2H) EXAMPLE 50: 3-(4-Aminobutyl)-4-hydroxy-1-[(2-naphthalen-2-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 50 is obtained from intermediate 40 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.9 (d, 1H), 7.9 / 7.85 (2*m, 2H), 7.7 (s, 1H), 7.6-7.4 (m, 5H), 7.3 (sts, 2 hrs), 4.35 / 4.2 (2dd, 2 hrs), 3.4-3.2 (sts, 1 hrs), 3.15-2.9 (sts, 2 hrs), 2.8 (sts, 2 hrs), 2.7 (dd, 1 H), 2 (m, 1H), 1.75 (m, 1H), 1.65-1.35 (m, 3H), 1.25 (m, 1H), 0.85 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 467.2090 (467.2099) Elemental Analysis: C=67.58(66.94);H=6.40(6.70);N=5.73(6.00) Intermediate 41: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[[2-( tert-Butyl 2,6-dichlorophenyl)phenyl]methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 41 is obtained from intermediates 21 and 242 according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.65-7.5 (m, 3H), 7.5-7.3 (m, 3H), 7.1 (d, 1H), 4 (m, 2H), 3.45 (m, 2H), 3.25 (2*d, 2H), 2.85-2.1 (m, 4H), 2-1.75 (m, 4H), 1.6-1.15 (m, 2H), 1.45 / 1.4 (2*s, 27H), 1.25 (t, 3H), 0.95 (m, 2H) EXAMPLE 51: 3-(4-Aminobutyl)-1-[[2-(2,6-dichlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 51 is obtained from intermediate 41 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.6 (d, 1H), 7.5 / 7.2 (m, 3H), 7.5-7.3 (m, 2H), 7.12 (d, 1H), 3.38 / 3.21 (2*d, 2H), 2.82 / 2.38 (2*dd, 2H), 2.65 / 2.22 (2*m, 2H), 2.45 (t, 2H), 1.85 / 1.71 (2*m, 2 H), 1.7 / 1.35 (2*m, 2H), 1.32 / 0.8 (2*m, 2H), 1.32 / 0.8 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 485.1169 (485.1163) Elemental Analysis: C=54.71(54.44);H=5.14(5.61);N=5.81(5.77) Intermediate 42: tert-Butyl 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-methyl-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 42 is obtained from intermediate 21 and formaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 3.98 (m, 2H), 3.48 (m, 2H), 2.75 (m, 2H), 2.49 / 2.2 (2m, 2H), 2.01 (s , 3H), 1.92 (m, 4H), 1.5 (m, 2H), 1.45 / 1.4 (2s, 27H), 1.25 / 1 (2m, 2H), 1.2 (t, 3H) EXAMPLE 52: 3-(4-Aminobutyl)-4-hydroxy-1-methyl-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 52 is obtained from intermediate 42 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 3.7-3.5 (m, 2 H), 3.3 (t, 1 H), 3.2 (dd, 1 H), 3 (t, 2 H), 2.9 (s, 3 H), 2.3 (m, 1H), 2 (m, 1H), 1.75 (m, 1H), 1.7 (m, 2H), 1.5 (m, 1H), 1.4 / 1.25 (2m, 2 H) ESI / FIA / HR and MS / MS: [M+H]+ = 265.1300 (265.1317) Elemental Analysis: C=45.59(45.45);H=7.97(8.01);N=10.61(10.60) Intermediate 43: 3-{4-[Bis-(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy- tert-Butyl 4-oxo-l-(2-phenylethyl)-l,4-azaphosphinane-3-carboxylate Intermediate 43 is obtained from intermediate 21 and phenylacetaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.3-7.15 (m, 5H), 3.98 (m, 2H), 3.45 (t, 2H), 3.05- 2.3 (m, 8H), 2 -1.8 (m, 4H), 1.4 (m+2s, 29H), 1.2 (t, 3H), 1.18 / 0.9 (2m, 2H) EXAMPLE 53: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-(2-phenylethyl)-1,4-azaphosphinane-3-carboxylic acid Example 53 is obtained from intermediate 43 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.4-7.25 (m, 5 H), 3.7 / 3.3 (2m, 2 H), 3.52 (m, 1 H), 3.45 (t, 2 H), 3.1 (m , 3H), 2.95 (m, 2H), 2.2 / 1.75 (2m, 2H), 1.95 (m, 1H), 1.62 (m, 2H), 1.5-1.1 (m, 3H) ESI / FIA / HR and MS / MS: [M+H]+ = 355.1777 (355.1786) Elemental Analysis C=57.63(57.62);H=7.36(7.68);N=7.90(7.90) Intermediate 44: tert-Butyl 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-pentyl-1,4-azaphosphinane-3-carboxylate Intermediate 44 is obtained from intermediate 21 and 1-pentanal according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 3.98 (m, 2H), 3.8 (m, 2H), 3.49 (t, 2H), 2.85 (m, 2H), 2.49 / 2.25 (2m , 2H), 1.9 (m, 4H), 1.45 / 1.4 (2s, 27H), 1.45 (m, 4H), 1.25 / 1 (2m, 6H), 1.2 (t, 3H), 0.85 (t, 3H) EXAMPLE 54: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-pentyl-1,4-azaphosphinane-3-carboxylic acid Example 54 is obtained from intermediate 44 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 3.7-3.5 (m, 2 H), 3.3 (m, 1 H), 3.15 / 3 (2m, 5 H), 2.27 (m, 1 H), 2 (m , 1H), 1.85-1.6 (m, 5H), 1.5 / 1.41 (2m, 2H), 1.3 (m, 5H), 0.85 (t, 3H) ESI / FIA / HR and MS / MS: [M+H]+ = 321.1923 (321.1943) Elemental Analysis: C=52.77(52.49);H=8.93(9.12);N=9.00(8.74) Intermediate 45: 3-{4-[Bis(tei"i-butoxycarbonyl)amino-butyl}-4-ethoxy-1-(naphthalen-1-ylmethyl)-4-oxo-1,4-azaphosphinane-3-carboxylate tert-butyl Intermediate 45 is obtained from intermediate 21 and 1-naphthaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.29 (d, 1H), 7.9 / 7.85 (2d, 2H), 7.6-7.4 (m, 4H), 3.95 (AB, 2H), 4 (m, 2H), 3.6 (m, 2H), 3.2-2.8 (m, 4H), 2.4 / 2 (2m, 2H), 1.7 (m, 2H), 1.4 / 1.3 (2s, 27 H), 1.22 (t, 3H), 1.05 / 0.75 (2m, 2H), 0.5 / 0.2 (2m, 2H) EXAMPLE 55: 3-(4-Aminobutyl)-4-hydroxy-1-(naphthalen-1-ylmethyl)-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 55 is obtained from intermediate 45 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.9 (m, 3H), 7.6-7.3 (m, 4H), 4.55 (s, 2H), 3.55 / 3.28 (2m, 2H), 3.4 / 3.15 (2dd, 2H), 2.75 (m, 2H), 2 / 1.6 (2m, 2H), 1.8 (m, 1H), 1.5-1.25 (m, 3H), 1 / 0.9 (2m, 2 h) ESI / FIA / HR and MS / MS: [M+H]+ = 391.1778 (391.1786) Elemental Analysis: C=61.34(61.53);H=6.58(6.97);N=7.01(7.18) Intermediate 46: tert-Butyl L-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-1-(cyclohexylmethyl)-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 46 is obtained from intermediate 21 and cyclohexanal according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 4 (m, 2 H), 3.5 (t, 2 H), 2.8 (m, 2 H), 2.48 / 2.25 (2m, 2 H), 2.15 (dd , 2H), 1.95 (m, 2H), 1.68 (m, 1H), 1.65 / 1.4 / 0.8 (3m, 10H), 1.45 (m, 3H), 1.45 / 1.4 (2s, 27H) , 1.2 (m, 2 H), 1.2 (t, 3 H), 1 (m, 1 H) EXAMPLE 56: 3-(4-Aminobutyl)-1-(cyclohexylmethyl)-4-hydroxy-4-oxo-acid l,4-azaphosphinane-3-carboxylic acid Example 56 is obtained from intermediate 46 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 3.7 / 3.25 (2m, 2H), 3.55 / 3.15 (2dd, 2H), 3.1-2.9 (t+2dd, 4H), 2.25 (m, 1H) , 2 (m, 1H), 1.85-1.55 (m, 9H), 1.52 / 1.41 (2m, 2H), 1.3 / 1.1 (m, 4H), 1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 347.2095 (347.2099) Elemental Analysis: C=55.29(55.48);H=9.08(9.02);N=7.95(8.09) Intermediate 47: 3-{4-Bis[tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-(naphthalen-2-ylmethyl)-4-oxo-1,4-azaphosphinane-3-carboxylate -butyl Intermediate 47 is obtained from intermediate 21 and 2-naphthaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.9 (m, 3H), 7.8 (s, 1H), 7.5 (m, 3H), 3.98 (m, 2H), 3.8 (d, 1 H), 3.6 (m, 3H), 3.35 / 3.2 (2m, 2H), 3.1-2.75 (2m, 2H), 2.4 (m, 1H), 2.05-1.8 (m, 3H), 1.4 -0.7 (m, 4H), 1.38 (3s, 27H), 1.22 (t, 3H) EXAMPLE 57: 3-(4-Aminobutyl)-4-hydroxy-1-(naphthalen-2-ylmethyl)-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 57 is obtained from intermediate 47 according to procedure D previously described. NMR Ή: (400 MHz, D20) δ ppm 7.95-7.9 (m, 4H), 7.6-7.5 (m, 3H), 4.5;4.3 (d, 2* 1H H), 3.65 (m, 1H) , 3.45-3.3 (m, 2H), 3.15 (m, 1H), 2.8 (m, 2H), 2.25 (m, 1H), 1.9-1.7 (m, 2H), 1.55-1.4 (m , 3H), 1.15-0.95 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 391.1778 (391.1786) Elemental Analysis: C=61.31(61.53);H=6.56(6.97);N=7.15(7.18) Intermediate 48: 3-{4-[Bis(f6-butoxycarbonyl)amino]butyl}-1-[(4-chlorophenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate tert-butyl Intermediate 48 is obtained from intermediate 21 and 4-chlorobenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.4 (d, 2H), 7.31 (d, 2H), 3.98 (m, 2H), 3.65-3.3 (m, 4H), 3-2.3 (m, 4H), 2-1.8 (m, 4H), 1.4 (s+m, 29H), 1.22 (2t, 3H), 0.8 (m, 2H) EXAMPLE 58: Acid 3-(4 -aminobutyl)-1-[(4-chlorophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic Example 58 is obtained from intermediate 48 according to procedure D previously described. NMR Ή: (400 MHz, D20) δ ppm 7.5 / 7.45 (2d, 4H), 4.41 / 4.21 (2d, 2H), 3.7 / 3.33 (2m, 2H), 3.45 / 3.1 (2dd, 2H) , 2.95 (m, 2H), 2.25 / 1.78 (2m, 2H), 1.95 / 1.5 (2m, 2H), 1.6 (m, 2H), 1.25 / 1.1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 375.1242 (375.1240) Elemental Analysis: C=50.89(51.27);H=6.01(6.45);N=7.44(7.47) Intermediate 49: Terf 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-fluorophenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylate -butyl Intermediate 49 is obtained from intermediate 21 and 4-fluorobenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.35 (m, 2H), 7.15 (t, 2H), 4 (m, 2H), 3.65-3.3 (m, 4H), 3-2.3 (m, 4H), 2-1.8 (m, 4H), 1.4 (s+m, 29H), 1.2 (2t, 3H), 0.9 / 0.8 ​​(2m, 2H) EXAMPLE 59: 3-(4-Aminobutyl)-1-[(4-fluorophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 59 is obtained from intermediary 49 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.5 (dd, 2 H), 7.2 (t, 2 H), 4.41 / 4.21 (2d, 2 H), 3.7 / 3.31 (2m, 2 H), 3.45 / 3.1 (2dd, 2H), 2.95 (m, 2H), 2.25 / 1.78 (2m, 2H), 1.95 / 1.5 (2m, 2H), 1.6 (m, 2H), 1.25 / 1.1 (2m, 2 h) ESI / FIA / HR and MS / MS: [M+H]+ = 359.1532 (359.1535) Elemental Analysis: C=53.65(53.63);H=6.20(6.75);N=7.83(7.82) Intermediate 50: tert- butyl Intermediate 50 is obtained from intermediate 21 and 2-furaldehyde according to procedure F previously described. 1H NMR: (400 MHz, CDC13) δ ppm 7.41 (s, 1 H), 6.32 (s, 1 H), 6.2 (s, 1 H), 4.09 (s, 2 H), 3.62 / 3.52 (AB, 2 H), 3.5 (m, 2H), 3 / 2.65 (m, 2H), 2.96 / 2.52 (m, 2H), 2.7-1.8 (m, 4H), 1.5 / 1.46 (m, 30H) , 1.3 (t, 3H), 1.01 (m, 1H) NMR 31 P: (400 MHz, CDC13) δ ppm 46.14 EXAMPLE 60: 3-(4-Aminobutyl)-1-(furan-2-ylmethyl)-4-hydroxy-4-azaphosphinane-3-carboxylic acid Example 60 is obtained from intermediate 50 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.6 (si, 1 H), 6.7 (tf, 1 H), 6.5 (tf, 1 H), 4.45 / 4.32 (2d, 2 H), 3.7 / 3.3 (2 *m, 2H), 3.52 / 3.12 (2*m, 2H), 2.98 (m, 2H), 2.25 / 1.8 (2*m, 2H), 1.95 / 1.5 (2*m, 2H) , 1.62 (m, 2H), 1.32 / 1.2 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 331.1422 (331.1422) Elemental Analysis: C=50.48(50.91);H=6.48(7.02);N=8.37(8.48) Intermediate 51: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[[4-(trifluoroomethyl)phenyl]methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 51 is obtained from intermediate 21 and 4-trifluoromethylbenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.71 (d, 2H), 7.52 (d, 2H), 4.03 (m, 2H), 3.72 / 3.51 (2*d, 2H), 3.35 (m, 2H), 3-2.3 (m, 4H), 1.98 (m, 4H), 1.4 (s+m, 29H), 1.2 (t, 3H), 0.8 (m, 2H) EXAMPLE 61: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[4- (trifluor omethyl)phenyl]methyl]-1,4-azaphosphinane-3-carboxylic acid Example 61 is obtained from intermediate 51 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.8 (d, 2 H), 7.65 (d, 2 H), 4.5 / 4.3 (AB, 2 H), 3.7 / 3.45 (m, 2 H), 3.39 / 3.11 (m, 2H), 2.9 (m, 2H), 2.28 / 1.8 (m, 2H), 1.95 / 1.49 (m, 2H), 1.6 (m, 2H), 1.2 / 1.1 (m, 2 h) NMR 19 F: (400 MHz, D20) δ ppm -62.5 NMR 31 P: (400 MHz, D20) δ ppm 24 ESI / FIA / HR and MS / MS: [M+H]+ = 409.1510 (409.1504) Elemental Analysis: C=49.86(50.00);H=5.32(5.92);N=6.83(6.86) Intermediate 52: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-methoxyphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylate -butyl Intermediate 52 is obtained from intermediate 21 and 4-methoxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.2 (d, 2H), 6.9 (d, 2H), 3.98 (m, 2H), 3.72 (s, 3H), 3.6 / 3.32 (2 *d, 2H), 3.4 (m, 2H), 3-2.25 (m, 4H), 1.9 (m, 4H), 1.4 (s+m, 29H), 1.2 (t, 3H) , 0.8 (m, 2H) EXAMPLE 62: 3-(4-Aminobutyl)-4-hydroxy-1-[(4-methoxyphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 62 is obtained from intermediate 52 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.41 (d, 2 H), 7.02 (d, 2 H), centered at 4.25 (AB, 2 H), 3.8 (s, 3 H), 3.7 / 3.3 (2m , 2H), 3.45 / 3.08 (2dd, 2H), 2.95 (m, 2H), 2.25 / 1.75 (2m, 2H), 1.95 / 1.45 (2m, 2H), 1.6 (m, 2H) , 1.25 / 1.1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 371.1712 (371.1730) Elemental Analysis: C=54.93(55.13);H=7.41(7.35);N=7.56(7.56) Intermediate 53: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4 -oxo-l- tert-Butyl (thiophen-3-ylmethyl)-l,4-azaphosphinane-3-carboxylate Intermediate 53 is obtained from intermediate 21 and 3-thiophenaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.49 (m, 1H), 7.31 (m, 1H), 7.02 (m, 1H), 3.95 (m, 2H), 3.6 / 3.49 (AB , 2H), 3.4 (m, 2H), 3 / 2.8 (m, 2H), 2.8 / 2.45 (m, 2H), 1.9 (m, 4H), 1.4 (m, 29H), 1.2 (t, 3H), 0.95 / 0.85 (m, 2H) NMR 31 P: (400 MHz, dmso-d6) δ ppm 47 / 45 EXAMPLE 63: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-(thiophen-3-ylmethyl)-1,4-azaphosphinane-3-carboxylic acid Example 63 is obtained from intermediate 53 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.61 (d, 1 H), 7.54 (dd, 1 H), 7.2 (d, 1 H), 4.42 / 4.28 (2*d, 2 H), 3.71 / 3.32 (m, 2H), 3.48 / 3.06 (m, 2H), 2.94 (m, 2H), 2.25 / 1.77 (m, 2H), 1.93 / 1.46 (m, 2H), 1.6 (m, 2 H), 1.26 / 1.13 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 347.1182 (347.1189) Elemental Analysis: C=48.14(48.55);H=6.55(6.69);N=7.87(8.09);S=8.65(9.26) Intermediate 54: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-hydroxy-3-methoxyphenyl)methyl]-4-oxo-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 54 is obtained from intermediate 21 and 4-hydroxy-3-methoxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.8 (s, 1H), 6.8 (df, 1H), 6.7 (d, 1H), 6.62 (dd, 1H), 3.95 (m, 2 H), 3.71 (s, 3H), 3.49 / 3.31 (2d, 2H), 3.4 (m, 2H), 3-2.2 (m, 4H), 2-1.8 (m, 4H), 1.4 (2s+m, 29H), 1.2 (2t, 3H), 1 / 0.85 (2m, 2H) EXAMPLE 64: 3-(4-Aminobutyl)-4-hydroxy-1-[(4-hydroxy-3-methoxyphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 64 is obtained from intermediate 54 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.09 (m, 1 H), 6.94 (m, 2 H), 4.3 / 4.13 (2*d, 2 H), 3.7 / 3.3 (2*m, 2 H) , 3.65 (s, 3H), 3.45 / 3.07 (2*m, 2H), 2.92 (m, 2H), 2.22 / 1.77 (2*m, 2H), 1.92 / 1.6 (2*m, 2 H), 1.6 / 1.48 (2*m, 2H), 1.23 / 1.11 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 387.1665 (387.1685) Elemental Analysis: C=53.10(52.85);H=7.01(7.04);N=7.30(7.25) Intermediate 55: Terf 3-{4-[Bis(tert-butoxycarbonyl)amino]butyl}-1-[(2-carboxyphenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate -butyl Intermediate 55 is obtained from intermediate 21 and methyl 2-formylbenzoate according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.65 (d, 1H), 7.5 (t, 1H), 7.38 (m, 2H), 4.05 / 3.4 (2d, 2H), 3.95 (m , 2H), 3.8 (2s, 3H), 3.3 / 3.2 (2m, 2H), 3-2.35 (m, 4H), 2 (m, 1H), 1.8-1.6 (m, 3H) , 1.4 / 1.3 (2s+m, 29H), 1.2 (2t, 3H), 0.5 / 0.35 (2m, 2H) EXAMPLE 65: 3-(4-Aminobutyl)-1-[(2-carboxyphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 55 is obtained from intermediate 65 according to procedure D previously described. ESI / FIA / HR and MS / MS: [M+H]+ = 385.1504 (385.1523) Elemental Analysis: C=53.42(53.12);H=6.25(6.56);N=7.40(7.29) Intermediate 56: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-l-[(3 tert-Butyl -chloro-4- hydroxyphenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 56 is obtained from intermediate 21 and 3-chloro-4-hydroxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 10.05 (m, 1H), 7.22 (df, 1H), 7.02 (dd, 1H), 6.9 (d, 1H), 3.98 (m, 2 H), 3.5 / 3.31 (2d, 2H), 3.4 (m, 2H), 3-2.25 (m, 4H), 2-1.8 (m, 4H), 1.4 (2s+m, 29H) , 1.2 (2t, 3H), 1.1-0.8 (2m, 2H) EXAMPLE 66: 3-(4-Aminobutyl)-1-[(3-chloro-4-hydroxyphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 66 is obtained from intermediate 56 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.42 (df, 1H), 7.2 (dd, 1H), 6.97 (d, 1H), 4.27 / 4.07 (2*d, 2H), 3.62 / 3.22 (2*m, 2H), 3.39 / 3 (2*m, 2H), 2.85 (m, 2H), 2.18 / 1.7 (2*m, 2H), 1.85 / 1.52 (2*m, 2 H), 1.52 / 1.4 (2*m, 2H), 1.18 / 1.05 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 391.1189 (391.1189) Elemental Analysis: C=49.09(49.17);H=6.02(6.19);N=7.18(7.17) Intermediate 57: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-hydroxy-3-(trifluor omethoxy)phenyl]methyl]-4-oxo-1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 57 is obtained from intermediate 21 and 4-hydroxy-3-(trifluoromethyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 10.1 (m, 1H), 7.15 (df, 1H), 7.08 (dd, 1H), 6.95 (d, 1H), 3.98 (m, 2 h), 3.5 / 3.4 (2d, 2 hrs), 3.4 (sts, 2 hrs), 3-2.2 (sts, 4 hrs), 2-1.8 (sts, 4 hrs), 1.4 (2s+m, 29 hrs) , 1.2 (2t, 3H), 1.1-0.8 (2m, 2H) EXAMPLE 67: 3-(4-Aminobutyl)-4-hydroxy-1-[[4-hydroxy-3-(trifluoromethoxy)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 67 is obtained from intermediate 57 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.44 (df, 1 H), 7.33 (dd, 1 H), 7.09 (d, 1 H), 4.38 / 4.13 (2*d, 2 H), 3.7 / 3.31 (2*dd, 2H), 3.44 / 3.07 (2*dd, 2H), 2.92 (m, 2H), 2.23 / 1.78 (2*m, 2H), 1.94 / 1.59 (2*m, 2H), 1.59 / 1.46 (2*m, 2H), 1.21 / 1.1 (2*m, 2H) NMR 19 F: (400 MHz, D20) δ ppm -58.3 NMR 31 P: (400 MHz, D20) δ ppm 26 ESI / FIA / HR and MS / MS: [M+H]+ = 441.1403 (441.1402) Elemental Analysis: C=46.46(46.37);H=4.98(5.49);N=6.42(6.36) Intermediate 58: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-hydroxy-3,5-dimethylphenyl)methyl]-4-oxo-1,4 tert-Butyl -azaphosphinane-3-carboxylate Intermediate 58 is obtained from intermediate 21 and 3,5-dimethyl-4-hydroxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.09 (s, 1H), 6.8 (s, 2H), 3.98 (m, 2H), 3.49 / 3.21 (2d, 2H), 3.35 (m , 2 hrs), 3-2.2 (m, 4 hrs), 2.15 (s, 6 hrs), 2-1.8 (m, 4 hrs), 1.4 (2s+m, 29 hrs), 1.2 (2t, 3 hrs) , 0.95-0.82 (2m, 2H) EXAMPLE 68: 3-(4-Aminobutyl)-4-hydroxy-1-[(4-hydroxy-3,5-dimethylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 68 is obtained from intermediate 58 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.1 (s, 2 H), 4.25-4.1 (d, 2 H), 3.7-3.5 (m, 2 H), 3.25 (m, 1 H), 3.1 (m , 1H), 2.95 (t, 2H), 2.2 (s, 6H), 2.2 / 1.75 (m, 2H), 1.95 (m, 1H), 1.6 (m, 2H), 1.5 (m , 1H), 1.3-1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 385.1889 (385.1892) Elemental Analysis: C=55.50(56.24);H=7.07(7.60);N=7.16(7.29) Intermediate 59: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo -I- tert-Butyl (pyridin-4-ylmethyl)-l,4-azaphosphinane-3-carboxylate Intermediate 59 is obtained from intermediate 21 and 4-formylpyridine according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.5 (d, 2H), 7.3 (d, 2H), 4.1-3.9 (2m, 2H), 3.65 / 3.52 (2x2d, 2H), 3.45 (2m, 2h), 2.95-2.3 (m, 4h), 1.98 (m, 4h), 1.5-1.35 (m+s, 29h), 1.22 (2t, 3h), 1.05 (m, 2 H) EXAMPLE 69: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-(pyridin-4-ylmethyl)-1,4-azaphosphinane-3-carboxylic acid Example 69 is obtained from intermediate 59 according to procedure D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.5 (d, 2H), 8.05 (m, 3H), 7.3 (d, 2H), 3.55 (AB, 2H), 3.05 / 2.3 (2m , 2H), 2.7 (m, 3H), 2.5 (m, 1H), 1.75 (m, 1H), 1.65-1.15 (m, 7H) ESI / FIA / HR and MS / MS: [M+H]+ = 342.1577 (342.1582) Elemental Analysis: C=52.56(52.78);H=6.70(7.09);N=12.22(12.31) Intermediate 60: tert- butyl Intermediate 60 is obtained from intermediate 21 and 3-formylpyridine according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.5 (d+s, 2H), 7.7 (2dd, 1H), 7.35 (m, 1H), 4.1-3.9 (2m, 2H), 3.65 / 3.52 (2x2d, 2 hrs), 3.45 (2m, 2 hrs), 3-2.3 (m, 4 hrs), 1.9 (m, 4 hrs), 1.4 (m+s, 30 hrs), 1.22 (2t, 3 H), 0.82 (m, 1H) EXAMPLE 70: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-(pyridin-3-ylmethyl)-1,4-azaphosphinane-3-carboxylic acid Example 70 is obtained from intermediate 60 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.6 (s+d, 2 H), 8 (dd, 1 H), 7.52 (dd, 1 H), 4.4 (AB, 2 H), 3.7 (m, 1 H), 3.4 (m, 2H), 3.18 (dd, 1H), 2.9 (m, 2H), 2.28 / 1.8 (2m, 2H), 1.91 (m, 1H), 1.6 (m, 2 H), 1.5 (m, 1H), 1.21 / 1.1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 342.1568 (342.1582) Elemental Analysis: C=52.32(52.78);H=6.66(7.09);N=12.32(12.31) Intermediate 61: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4 -oxo-l- tert-Butyl (pyridin-2-ylmethyl)-l,4-azaphosphinane-3-carboxylate Intermediate 61 is obtained from intermediate 21 and 2-formylpyridine according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.5 (df, 1H), 7.75 (t, 1H), 7.42 / 7.25 (2dd, 2H), 4.1- 3.9 (2m, 2H), 3.71 / 3.6 (2AB, 2H), 3.5-3.35 (m, 2H), 3-2.3 (m, 4H), 2.0-2.9 (m, 4H), 1.45 / 1.35 (3s, 27H), 1.4 / 1-0.8 (3m, 4H), 1.22 (2t, 3H) EXAMPLE 71: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-(pyridin-2-ylmethyl)-1,4-azaphosphinane-3-carboxylic acid Example 71 is obtained from intermediary 61 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.6 (dd, 1 H), 7.91 (t, 1 H), 7.55 (d, 1 H), 7.45 (dd, 1 H), centered at 4.41 (AB, 2 H), 3.75 / 3.4 (2m, 2H), 3.55 / 3.3 (2dd, 2H), 2.95 (m, 2H), 2.3 / 1.78 (2m, 2H), 1.98 (m, 1H), 1.65 (m, 2H), 1.5 (m, 1H), 1.3 / 1.2 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 342.1592 (342.1582) Elemental Analysis: C=52.72(52.78);H=6.92(7.09);N=12.25(12.31) Intermediate 63: tert- butyl Intermediate 63 is obtained from intermediate 21 and 2-cyclohexylacetaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 3.98 (m, 2H), 3.48 (t, 2H), 2.8 (m, 2H), 2.5-2.2 (m, 4H), 2-0.8 (m, 19H), 1.9 (m, 2H), 1.45 / 1.4 (2s, 27H), 1.2 (t, 3H) EXAMPLE 73: 3-(4-Aminobutyl)-1-(2-cyclohexylethyl)-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 73 is obtained from intermediate 63 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 3.7-3.5 (m, 2 H), 3.3 (m, 1 H), 3.15 (m, 3 H), 3 (t, 2 H), 2.22 / 1.8 (2m , 2H), 2 (m, 1H), 1.7-0.85 (m, 17H), 1.65 (m, 1H) ESI / FIA / HR and MS / MS: [M+H]+ = 361.2257 (361.2256) Elemental Analysis: C=56.25(56.65);H=8.92(9.23);N=7.49(7.77) Intermediate 64: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4 tert-butyl -oxo-l-[(4-phenylphenyl)methyl]-l,4-azaphosphinane-3-carboxylate Intermediate 64 is obtained from intermediate 21 and 4-phenylbenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.69 (2d, 4H), 7.5-7.3 (m, 5H), 4 (m, 2H), 3.7 / 3.45 (2d, 2H), 3.4 (m, 2H), 3.05-2.3 (m, 4H), 2.05-1.65 (m, 4H), 1.4 (m+2s, 29H), 1.22 (2t, 3H), 1-0.7 (m , 2H) EXAMPLE 74: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(4-phenylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 74 is obtained from intermediate 64 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.8 (d, 2 H), 7.7 (d, 2 H), 7.55 (d, 2 H), 7.5 (t, 2 H), 7.41 (t, 1 H) , 4.45 / 4.28 (2d, 2h), 3.75 / 3.35 (2m, 2h), 3.5 / 3.15 (2dd, 2h), 2.9 (m, 2h), 2.25 / 1.8 (2m, 2h), 1.95 / 1.45 (2m, 2H), 1.6 (m, 2H), 1.25 / 1.1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 417.1932 (417.1943) Elemental Analysis: C=63.25(63.45);H=6.64(7.02);N=6.55(6.73) Intermediate 65: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4 tert-butyl -oxo-l-[(3-phenoxyphenyl)methyl]-l,4-azaphosphinane-3-carboxylate Intermediate 65 is obtained from intermediate 21 and 3-phenoxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.38 (2t, 3H), 7.15 (t, 1H), 7.05 (d, 1H), 7.05 (d, 2H), 6.95 (si, 1 H), 6.9 (d, 1H), 3.98 (m, 2H), 3.6 / 3.45 (2d, 2H), 3.4 (m, 2H), 3-2.3 (m, 4H), 2-1.6 (m, 6H), 1.4 (2s, 27H), 1.2 (2t, 3H), 1-0.75 (m, 2H) EXAMPLE 75: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(3-phenoxyphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 75 is obtained from intermediary 65 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.5-7.3 (2t, 3H), 7.2-6.95 (m, 6H), centered at 4.2 (AB, 2H), 3.65 / 3.25 (2m, 2H) , 3.4 / 3 (2dd, 2H), 2.82 (m, 2H), 2.19 / 1.7 (2m, 2H), 1.88 / 1.4 (2m, 2H), 1.52 (m, 2H), 1.2-1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 433.1891 (433.1892) Elemental Analysis: C=60.90(61.10);H=6.58(6.76);N=6.34(6.48) Intermediate 66: tert-butyl 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-(3-phenylpropyl)-1,4-azaphosphinane-3-carboxylate Intermediate 66 is obtained from intermediate 21 and 3-phenylpropanal according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.29 (t, 2H), 7.15 (d+t, 3H), 3.98 (m, 2H), 3.49 (t, 2H), 2.9-2.2 (m, 4H), 2.59 (t, 2H), 2.35 (m, 2H), 2-1.6 (m, 7H), 1.5 (m, 1H), 1.4 (2s, 27H), 1.25 / 1 (2m, 2H), 1.2 (2t, 3H) EXAMPLE 76: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-(3-phenylpropyl)-1,4-azaphosphinane-3-carboxylic acid Example 76 is obtained from intermediate 66 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.38 (t, 2 H), 7.27 (m, 3 H), 3.62 / 3.28 (2m, 2 H), 3.52 (dd, 1H), 3.11 (m, 3H), 3 (td, 2H), 2.7 (t, 2H), 2.25 / 1.75 (2m, 2H), 2.09 (m, 2H), 1.95 / 1.5 ( 2m, 2H), 1.65 (m, 2H), 1.38 / 1.22 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 369.195 (369.1943) Elemental Analysis: C=58.46(58.68);H=7.45(7.93);N=7.54(7.60) Intermediate 68: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4 tert-butyl -oxo-l-[(4-phenoxyphenyl)methyl]-l,4-azaphosphinane-3-carboxylate Intermediate 68 is obtained from intermediate 21 and 4-phenoxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.4 (t, 2H), 7.3 (d, 2H), 7.12 (t, 1H), 6.98 (2d, 4H), 3.99 (m, 2 H), 3.6 / 3.4 (2d, 2H), 3.38 (m, 2H), 3-2.25 (m, 4H), 2-1.65 (m, 6H), 1.4 (2s, 27H), 1.2 (2t, 3H), 1-0.75 (m, 2H) EXAMPLE 78: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(4-phenoxyphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 78 is obtained from intermediary 68 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.44 (d, 2H), 7.41 (t, 2H), 7.21 (t, 1H), 7.08 (d, 2H), 7.08 (d, 2H) , 4.38 / 4.21 (2d, 1+1H), 3.7 / 3.31 (m+m, 1+1H), 3.5 / 3.1 (2d, 2H), 2.93 (m, 2H), 2.23 / 1.77 (m +m, 1+1H), 1.93 / 1.48 (m+m, 1+1H), 1.6 (quint., 2H), 1.24 / 1.13 (m+m, 1+1H) NMR 13 C: (400 MHz, D20) δ ppm 177.6, 158.2, 155.7, 132.1, 130, 124.3, 124.1, 119.3, 118.7, 59.4, 51.6, 50.9, 38.8, 27, 26.6, 24.8, 20 NMR 31 P: (400 MHz, D20) δ ppm 25 ESI / FIA / HR and MS / MS: [M+H]+ = 433.1884 (433.1892) Elemental Analysis: C=60.77(61.10);H=6.27(6.76);N=6.42(6.48) EXAMPLE 79: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-(2-phenylmethoxyethyl)-1,4-azaphosphinane-3-carboxylic acid Example 79 is obtained from intermediate 21 and benzyloxyacetaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.42 (m, 5 H), 4.63 (d, 1 H), 4.55 (d, 1 H), 3.82 (t, 2 H), 3.61 (dd, 1 H) , 3.5 (m, 1H), 3.33 (m, 2H), 3.26 (m, 1H), 3.16 (dd, 1H), 2.92 (t, 2H), 2.24 (m, 1H), 1.94 (m, 1H), 1.71 (m, 1H), 1.61 (quint, 2H), 1.48 (m, 1H), 1.21 (m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 25.6 ESI / FIA / HR and MS / MS: [M+H]+ = 385.1883 (385.1892) EXAMPLE 80: 3-(4-Aminobutyl)-4-hydroxy-1-(2-hydroxyethyl)-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 80 is obtained from example 79 according to procedure E previously described. 1H NMR: (400 MHz, D20) δ ppm 3.9 (m, 2 H), 3.72 (dd, 1 H), 3.62 (dd, 1 H), 3.32 (m, 1 H), 3.29 (t, 2 H) , 3.25 (dd, 1H), 2.99 (m, 2H), 2.29 (m, 1H), 1.99 (m, 1H), 1.79 (m, 1H), 1.67 (quint, 2H), 1.52 (m, 1H), 1.41 (m, 1H), 1.29 (m, 1H) ESI / FIA / HR and MS / MS: [M+H]+ = 295.1424 (295.1422) Elemental Analysis: C=44.08(44.90);H=7.66(7.88);N=9.23(9.52) Intermediate 69: Terf 3-{4-[Bis(tert-butoxycarbonyl)amino]butyl}-1-[(3-chlorophenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate -butyl Intermediate 69 is obtained from intermediate 21 and 3-chlorobenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.4-7.2 (m, 4H), 3.99 (m, 2H), 3.62 / 3.43 (AB, 1+1H), 3.38 (m, 2H) , 2.92 / 2.36 (m)+(m, 1+1H), 2.73 / 2.47 (m)+(m, 1+1H), 1.96 (m, 2H), 1.89 (m, 2H), 1.41 (m, 2H), 1.37 / 1.33 (2*(s, 27H), 1.2 (t, 3H), 0.81 (m, 2H) NMR 13 C: (400 MHz, dmso-d6) δ ppm 127-130, 152.3, 60.9, 60.6, 54.9, 51.6, 45.6, 28.9, 28.9, 27.6, 24.7, 20.6, 133.2, 81.8 / 81.1 EXAMPLE 81: 3-(4-Aminobutyl)-1-[(3-chlorophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 81 is obtained from intermediary 69 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.52-7.35 (m, 4H), centered at 4.32 (AB, 2H), 3.7 / 3.32 (2m, 2H), 3.5 / 3.12 (2dd, 2H) , 2.93 (m, 2H), 2.25 / 1.8 (2m, 2H), 1.95 / 1.48 (2m, 2H), 1.6 (m, 2H), 1.25 / 1.11 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 375.1256 (375.1240) Elemental Analysis: C=51.26(51.27);H=6.32(6.45);N=7.43(7.47) Intermediate 70: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(3-hydroxyphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylate of terf-butyl Intermediate 70 is obtained from intermediate 21 and 3-hydroxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.25 (s, 1H), 7.1 (t, 1H), 6.7-6.55 (m, 3H), 3.98 (m, 2H), 3.52 / 3.4 (2d, 2H), 3.4 (m, 2H), 3-2.2 (m, 4H), 2-1.65 (m, 6H), 1.4 (2s, 27H), 1.2 (2t, 3H), 0.95 / 0.82 (2m, 2H) EXAMPLE 82: 3-(4-Aminobutyl)-4-hydroxy-1-[(3-hydroxyphenyl)methyl]-4-1,4-azaphosphinane-3-carboxylic acid Example 82 is obtained from intermediate 70 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.38 (t, 1 H), 7-6.9 (m, 3 H), centered at 4.18 (AB, 2 H), 3.7 / 3.32 (2m, 2 H), 3.45 / 3.1 (2dd, 2H), 2.91 (m, 2H), 2.25 / 1.8 (2m, 2H), 1.92 / 1.48 (2m, 2H), 1.6 (m, 2H), 1.25 / 1.1 (2m , 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 357.1573 (357.1579) Elemental Analysis: C=53.22(53.93);H=6.98(7.07);N=7.72(7.86) Intermediate 71: terf -butyl Intermediate 71 is obtained from intermediate 21 and 4-hydroxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.25 (s, 1H), 7.05 (d, 2H), 6.7 (d, 2H), 3.98 (m, 2H), 3.49 / 3.3 (2d , 2 hrs), 3.4 (m, 2 hrs), 3-2.2 (m, 4 hrs), 2-1.8 (m, 4 hrs), 1.4 (2s+m, 29 hrs), 1.2 (2t, 3 hrs) , 0.95 / 0.82 (2m, 2H) EXAMPLE 83: 3-(4-Aminobutyl)-4-hydroxy-1-[(4-hydroxyphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 83 is obtained from intermediate 71 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.38 (d, 2 H), 6.95 (d, 2 H), centered at 4.25 (AB, 2 H), 3.7 / 3.3 (2m, 2 H), 3.48 / 3.05 (2dd, 2H), 2.95 (m, 2H), 2.21 / 1.75 (2m, 2H), 1.95 / 1.5 (2m, 2H), 1.6 (m, 2H), 1.25 / 1.11 (2m, 2 h) ESI / FIA / HR and MS / MS: [M+H]+ = 357.1572 (357.1579) Elemental Analysis: C=53.24(53.93);H=6.89(7.07);N=7.57(7.86) Intermediate 72: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-1-(furan-3-ylmethyl)-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate tert-butyl Intermediate 72 is obtained from intermediate 21 and 3-furaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.61 / 7.55 (2sl, 2H), 6.39 (si, 1H), 3.98 (m, 2H), 3.49 / 3.33 (2d, 2H), 3.45 (m, 2 hrs), 3-2.2 (m, 4 hrs), 2-1.8 (m, 4 hrs), 1.4 (2s+m, 29 hrs), 1.2 (2t, 3 hrs), 1.05 / 0.9 (2m , 2H) EXAMPLE 84: 3-(4-Aminobutyl)-1-(furan-3-ylmethyl)-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 84 is obtained from intermediate 72 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.71 (si, 1 H), 7.59 (si, 1 H), 6.58 (si, 1 H), centered at 4.22 (AB, 2 H), 3.7 / 3.35 (2m , 2H), 3.55 / 3.08 (2dd, 2H), 2.95 (m, 2H), 2.25 / 1.8 (2m, 2H), 1.95 / 1.5 (2m, 2H), 1.62 (m, 2H) , 1.31 / 1.18 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 331.1431 (331.1422) Elemental Analysis: C=50.45(50.91);H=6.72(7.02);N=8.39(8.48) Intermediate 73: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(2-hydroxyphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylate tert-butyl Intermediate 73 is obtained from intermediate 21 and 2-hydroxybenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.45 (s, 1H), 7.1 (d+t, 2H), 6.78 (d+t, 2H), 4 (m, 2H), 3.62 / 3.52 (2d, 2H), 3.4 (m, 2H), 3-2.3 (m, 4H), 2-1.8 (m, 4H), 1.42 / 1.38 (m+2s, 29H), 1.21 (2t, 3H), 0.98 / 0.85 (2m, 2H) EXAMPLE 85: 3-(4-Aminobutyl)-4-hydroxy-1-[(2-hydroxyphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 85 is obtained from intermediate 73 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.39 (t, 1 H), 7.3 (d, 1 H), 6.95 (d+t, 2 H), 4.28 (AB, 2 H), 3.65 / 3.28 (2m , 2H), 3.52 / 3.2 (2dd, 2H), 2.95 (m, 2H), 2.2 / 1.72 (2m, 2H), 1.98 / 1.5 (2m, 2H), 1.62 (m, 2H) , 1.3 / 1.18 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 357.1591 (357.1579) Elemental Analysis C=53.22(53.93);H=6.97(7.07);N=7.71(7.86) Intermediate 74: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(4-hydroxyphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 74 is obtained from intermediate 21 and 2-(4-hydroxyphenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.45 (s, 1H), 7.45 (dd, 1H), 7.3 (td, 2H), 7.16 (dd, 1H), 7.13 (d, 2 H), 6.81 (d, 2 H), 3.93 (quad., 2 H), 3.54 / 3.36 (d, 2 H), 3.28 (t, 2 H), 2.85-2.15 (m, 2 H), 2.85- 2.15 (m, 2H), 1.84 (m, 2H), 1.84 (m, 2H), 1.47-1.3 (s, 27H), 1.47-1.3 (s, 2H), 1.17 (t, 3H ), 0.7 (m, 2H) NMR 31 P: (400 MHz, dmso-d6) δ ppm 45.3 EXAMPLE 86: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(4-hydroxyphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 86 is obtained from intermediate 74 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.56 (dd, 1 H), 7.55-7.45 (2td, 2 H), 7.37 (dd, 1 H), 7.25 (d, 2 H), 7 (d, 2 H), 4.36 (dd, 2H), 3.35 / 3.1 (2m, 2H), 3.2 / 2.85 (2m, 2H), 2.95 (m, 2H), 2.05 / 1.65 (2m, 2H), 1.85 / 1.35 (2m, 2H), 1.6 (m, 2H), 1.2-0.95 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 433.1893 (433.1892) Elemental Analysis: C=61.11(61.10);H=6.10(6.76);N=6.68(6.48) Intermediate 75: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(3-phenyl-1H-pyrazol-4-yl)methyl]-1,4 tert-Butyl-azaphosphinane-3-carboxylate Intermediate 75 is obtained from intermediate 21 and 3-phenyl-1H-pyrazole-4-carboxaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 13-12.5 (m, 1H), 7.9-7.3 (m, 6H), 4.05-3.9 (m, 2H), 3.45 (dd, 2H) , 3.3 (m, 2H), 3.1-2.2 (m, 6H), 2-1.7 (m, 2H), 1.4 (s, 18H), 1.35 (s, 9H), 1.2 (m, 2 H), 1.2 (t, 3H), 1-0.7 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 691.3829 (691.3835) EXAMPLE 87: Acid 3-(4-aminobutyl)-4-hydroxy-4-oxo-1-[(3-phenyl-1H -pyrazol-4-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 87 is obtained from intermediate 75 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.95 (si, 1H), 7.6-7.5 (m, 5H), 4.45 (dd, 2H), 3.55 / 3.15 (2m, 2H), 3.05 / 2.7 (2m, 2H), 2.9 (m, 2H), 2.2 / 1.7 (m, 2H), 1.8 / 1.25 (2m, 2H), 1.5 (m, 2H), 0.95 / 0.7 (2m, 2 h) ESI / FIA / HR and MS / MS: [M+H]+ = 407.1865 (407.1848) Elemental Analysis: C=55.99(56.15);H=6.40(6.70);N=13.79(13.79) Intermediate 76: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(4-methoxyphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 76 is obtained from intermediate 21 and 2-(4-methoxyphenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.47 (d, 1H), 7.32 (m, 2H), 7.27 (d, 2H), 7.19 (d, 1H), 7 (d, 2 H), 3.93 (m, 2H), 3.8 (s, 3H), 3.54 / 3.37 (2*d, 2H), 3.32 (m, 2H), 2.74 / 2.22 (m, 2H), 2.74 / 2.33 (m, 2 hrs), 1.95-1.75 (m, 2 hrs), 1.95-1.75 (m, 2 hrs), 1.41 (s, 18 hrs), 1.37 (m, 2 hrs), 1.34 (s, 9 H), 1.18 (t, 3H), 0.7 (m, 2H) EXAMPLE 88: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(4-methoxyphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 88 is obtained from intermediate 76 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.59 (dd, 1H), 7.51 (m, 2H), 7.38 (dd, 1H), 7.31 (d, 2H), 7.1 (d, 2H) , 4.44 / 4.29 (2*d, 2H), 3.36 (s, 3H), 3.19 / 2.94 (m, 2H), 3.19 / 2.84 (m, 2H), 2.94 (m, 2H), 2.08 / 1.65 (m, 2H), 1.85 / 1.35 (m, 2H), 1.58 (m, 2H), 1.13 / 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 447.2046 (447.2048) Elemental Analysis: C=62.04(61.87);H=6.38(7.00);N=6.05(6.27) Intermediate 77: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(4-phenyl-1H-pyrazol-3-yl)methyl] - 1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 77 is obtained from intermediate 21 and 4-phenyl-1H-pyrazole-3-carboxaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 13-12.5 (m, 1H), 8 (m, 1H), 7.62 (d, 2H), 7.35 (t, 2H), 7.2 (t , 1H), 4.1-3.9 (m, 2H), 3.8-3.35 (m, 2H), 3.25 (m, 2H), 3.15-2.3 (m, 4H), 2.1-1.9 (m, 2 H), 1.8 (m, 2H), 1.4-1.2 (m, 2H), 1.4 (s, 18H), 1.35 (s, 9H), 1.2 (t, 3H), 0.7 (m, 2 h) EXAMPLE 89: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(4-phenyl-1H-pyrazol-3-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 89 is obtained from intermediate 77 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.9 (s, 1H), 7.55-7.35 (m, 5H), 4.65-4.4 (dd, 2H), 3.55 / 3.15 (2m, 2H), 3.15 / 2.9 (2m, 2H), 2.9 (m, 2H), 2.15 / 1.65 (2m, 2H), 1.8 / 1.25 (m, 2H), 1.5 (m, 2H), 0.95 / 0.75 (2m , 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 407.1844 (407.1848) Elemental Analysis: C=56.58(56.15);H=6.24(6.70);N=13.79(13.79) Intermediate 78: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(5-phenyl-1,3-oxazol-4-yl)methyl] - tert-butyl 1,4-azaphosphinane-3-carboxylate Intermediate 78 is obtained from intermediate 21 and 5-phenyl-1,3-oxazole-4-carboxaldehyde according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 8.29 (s, 1H), 7.78 (m, 2H), 7.5 (m, 2H), 7.4 (m, 1H), 4 (m, 2 H), 3.68 (dd, 2H), 3.3 (m, 2H), 3.05 / 2.5 (2m, 2H), 2.95 / 2.65 (2m, 2H), 2.05-1.7 (m, 4H), 1.45 (s, 6 hrs), 1.35 (s, 9 hrs), 1.25 (m, 2 hrs), 1.25 (t, 3 hrs), 0.9 (m, 2 hrs) EXAMPLE 90: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(5-phenyl-1,3-oxazol-4-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 90 is obtained from intermediate 78 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.28 (s, 1 H), 7.68 (d, 2 H), 7.6-7.5 (m, 3 H), 4.55 (dd, 2 H), 3.65 / 3.3 (2m , 2H), 3.4 / 3.1 (2dd, 2H), 2.9 (m, 2H), 2.2 / 1.71 (2m, 2H), 1.9 / 1.35 (2m, 2H), 1.55 (m, 2H) , 1.05 / 0.95 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 408.1689 (408.1688) Elemental Analysis: C=55.52(56.02);H=6.16(6.43);N=10.20(10.31) Intermediate 79: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(1,2-oxazol-5-yl)phenyl]methyl]-4- tert-butyl oxo-1,4-azaphosphinane-3-carboxylate Intermediate 79 is obtained from intermediates 21 and 218 according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 8.6 (d, 1H), 7.65 (m, 1H), 7.55-7.4 (m, 3H), 6.75 (d, 1H), 4 (m , 2H), 3.85 / 3.5 (dd, 2H), 3.3 (m, 2H), 2.95 / 2.4 (2m, 2H), 2.8 / 2.55 (2m, 2H), 2.1- 1.6 (2m, 4 H), 1.45 (s, 18H), 1.35 (m, 2H), 1.35 (s, 9H), 1.22 (t, 3H), 0.9-0.5 (m, 2H) EXAMPLE 91: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(1,2-oxazol-5-yl)phenyl]methyl]-4-oxo-1,4-azaphosphinan-3-acid carboxylic Example 91 is obtained from intermediate 79 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.55 (d, 1 H), 7.85 (m, 1 H), 7.65-7.55 (m, 3 H), 6.85 (d, 1 H), 4.7 / 4.4 (dd , 2H), 3.85 / 3.2 (2m, 2H), 3.5 / 3.2 (2dd, 2H), 2.9 (m, 2H), 2.3 / 1.8 (2m, 2H), 1.9 / 1.45 (2m, 2 H), 1.6 (m, 2H), 1.2 / 1.05 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 408.1685 (408.1688) Elementary Analysis: C=55.14(56.02);H=5.95(6.43);N=10.14(10.31) Intermediate 80: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-pyrazol-1-ylphenyl)methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 80 is obtained from intermediate 21 and 2-(1H-pyrazol-1-yl)-benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.04 (d, 1H), 7.7 (d, 1H), 7.55-7.35 (m, 4H), 6.5 (m, 1H), 3.95 (m , 2 hrs), 3.65 / 3.35 (dd, 2 hrs), 3.3 (m, 2 hrs), 2.8-2.6 (2m, 2 hrs), 2.4-2.15 (2m, 2 hrs), 2-1.65 (m, 4 H), 1.5-1.3 (m, 2H), 1.41 (s, 18H), 1.35 (s, 9H), 1.19 (t, 3H), 0.7 (m, 2H) EXAMPLE 92: Acid 3- (4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-pyrazol-1-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic Example 92 is obtained from intermediate 80 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.05 (d, 1H), 7.9 (d, 1H), 7.7-7.45 (m, 4H), 6.6 (t, 1H), 4.25 (dd, 2 H), 3.5 / 3.1 (2dd, 2H), 3.35 / 3.15 (2m, 2H), 2.95 (m, 2H), 2.3 / 1.8 (2m, 2H), 1.9 / 1.5 (2m, 2H) , 1.6 (m, 2H), 1.3 / 1.1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 407.1869 (407.1848) Elemental Analysis: C=56.00(56.15);H=6.16(6.70);N=13.77(13.79) Intermediate 81: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-fluoro-6-(4-methoxyphenyl)phenyl]methyl]-4-oxo- tert-Butyl 1,4-azaphosphinane-3-carboxylate Intermediate 81 is obtained from intermediate 21 and 2-fluoro-6-(4-methoxyphenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, D20) δ ppm 7.4 (d, 2 H), 7.4 (dd, 1 H), 7.18 (t, 1 H), 7.08 (d, 1 H), 7 (d, 2 H) , 3.92 (m, 2H), 3.8 (s, 3H), 3.46 (s, 2H), 3.22 (m, 2H), 2.7 / 2.38 (dd, 2H), 2.65 / 2.25 (2*m , 2H), 2-1.6 (m, 4H), 1.4 (s, 18H), 1.34 (s, 9H), 1.25 (m, 2H), 1.18 (t, 3H), 0.63 / 0.5 (2*m, 2H) EXAMPLE 93: 3-(4-Aminobutyl)-1-[[2-fluoro-6-(4-methoxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 93 is obtained from intermediate 81 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.54 (m, 1H), 7.3 (d, 2H), 7.28 (m, 1H), 7.21 (d, 1H), 7.11 (d, 2H) , 4.42 (dd, 2H), 3.86 (s, 3H), 3.46 / 3.09 (m, 2H), 3.2 / 2.9 (m, 2H), 2.95 (m, 2H), 2.11 / 1.67 (m , 2H), 1.87 / 1.37 (m, 2H), 1.6 (m, 2H), 1.11 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 465.1955 (465.1954) Elemental Analysis: C=59.31(59.48);H=5.75(6.51);N=6.10(6.03) Intermediate 82: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(1-methylpyrazol-4-yl)phenyl]methyl]-4-oxo- tert-Butyl 1,4-azaphosphinane-3-carboxylate Intermediate 82 is obtained from intermediates 21 and 235 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.9 (s, 1H), 7.65 (s, 1H), 7.4-7.35 (m, 2H), 7.3-7.2 (m, 2H), 4 (m, 2H), 3.9 (s, 3H), 3.61 / 3.4 (dd, 2H), 3.3-3.15 (m, 2H), 2.9 / 2.35 (2m, 2H), 2.8 / 2.45 (2dd , 2H), 2.05-1.9 (m, 2H), 1.8 (m, 2H), 1.4 (s, 18H), 1.35 (s, 9H), 1.25 (m, 2H), 1.2 (t , 3 H), 0.65 (m, 2 H) EXAMPLE 94: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(1-methylpyrazol-4-yl)phenyl]methyl]-4-acid oxo-1,4-azaphosphinane-3-carboxylic acid Example 94 is obtained from intermediate 82 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.75 (s, 1 H), 7.6 (s, 1 H), 7.55-7.35 (m, 4 H), 4.4 (dd, 2 H), 3.9 (s, 3 H), 3.6-3.1 (m, 3H), 3-2.8 (m, 3H), 2.05 / 1.7 (m, 2H), 1.85 / 1.35 (m, 2H), 1.55 (m, 2H) , 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 421.2016 (421.2004) Elemental Analysis: C=56.61(57.13);H=6.36(6.95);N=13.08(13.33) Intermediate 83: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-pyrimidin-5-ylphenyl)methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 83 is obtained from intermediates 21 and 236 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.2 (s, 1H), 8.86 (s, 2H), 7.5-7.3 (m, 4H), 3.93 (m, 2H), 3.46 (dd , 2H), 3.3 (m, 2H), 2.78-2.6 (2m, 2H), 2.4 (dd, 1H), 2.2 (m, 1H), 2-1.75 (m, 2H), 1.65 (m, 2H), 1.4 (m, 2H), 1.4 (s, 18H), 1.33 (s, 9H), 1.18 (t, 3H), 0.6 (m, 2H) EXAMPLE 95: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-pyrimidin-5-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 95 is obtained from intermediate 83 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 9.19 (s, 1 H), 8.85 (s, 2 H), 7.7 (m, 1 H), 7.68-7.59 (m, 2 H), 7.45 (m, 1H), 4.38 (dd, 2H), 3.52 / 3.15 (2m, 2H), 3.25 / 2.9 (2m, 2H), 2.9 (m, 2H), 2.1 / 1.7 (2m, 2H), 1.85 / 1.4 (2m, 2H), 1.6 (m, 2H), 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 419.1856 (419.1848) Elemental Analysis: C=57.94(57.41);H=6.37(6.50);N=13.40(13.39) Intermediate 84: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(2-methylpyrazol-3-yl)phenyl]methyl]-4-oxo- tert-Butyl 1,4-azaphosphinane-3-carboxylate Intermediate 84 is obtained from intermediates 21 and 280 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.56 (dd, 1H), 7.5 (d, 1H), 7.47 (td, 1H), 7.39 (td, 1H), 7.28 (dd, 1 H), 6.25 (d, 1H), 3.95 (m, 2H), 3.58 (s, 3H), 3.45-3.25 (m, 4H), 2.8 / 2.2 (2m, 2H), 2.7 / 2.35 (2dd, 2H), 2-1.75 (m, 4H), 1.4 (m, 2H), 1.4 (s, 18H), 1.35 (s, 9H), 1.2 (t, 3H), 0.7 (m, 2H) EXAMPLE 96: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(2-methylpyrazol-3-yl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 96 is obtained from intermediate 84 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.7-7.4 (m, 4 H), 7.63 (d, 1 H), 6.45 (d, 1 H), 4.2 (dd, 2 H), 3.58 (s, 3 H), 3.55-3.05 (m, 4H), 2.8 (m, 2H), 2.1 / 1.7 (2m, 2H), 1.85 / 1.4 (2m, 2H), 1.6 (m, 2H), 1.3 -1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 421.2019 (421.2004) Elemental Analysis: C=57.47(57.13);H=6.44(6.95);N=13.24(13.33) Intermediate 85: 3-{4-[Bis(ter^butoxycarbonyl)amino]butyl}-1-[[2-(2-chlorophenyl)phenyl]methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 85 is obtained from intermediates 21 and 214 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.56 (m, 1H), 7.56 / 7.49 (d, 1H), 7.42 (m, 2H), 7.42 (m, 1H), 7.34 (m , 1H), 7.27 (m, 1H), 7.12 (m, 1H), 3.92 (m, 2H), 3.5-3.15 (m, 2H), 3.5- 3.15 (m, 2H), 2.68 / 2.1 (m, 2H), 2.68 / 2.31 (m, 2H), 2-1.7 (m, 2H), 2-1.7 (m, 2H), 1.42 (s, 18H), 1.39 (m , 2H), 1.34 (s, 9H), 1.16 (2*t, 3H), 0.73 (m, 2H) EXAMPLE 97: 3-(4-Aminobutyl)-1-[[2-(2-chlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 97 is obtained from intermediate 85 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.7-7.25 (m, 4H), 7.7-7.25 (m, 4H), 4.45-3.9 (m, 2H), 3.75-3 (m, 2H) , 3.45-2.75 (m, 2H), 2.95 (m, 2H), 2.15 / 1.69 (m, 2H), 1.87 / 1.38 (m, 2H), 1.59 (m, 2H), 1.3-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 451.1545 (451.1553) Elemental Analysis: C=58.81(58.60);H=6.24(6.26);N=6.36(6.21) Intermediate 86: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(2-imidazol-1-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane tert-Butyl-3-carboxylate Intermediate 86 is obtained from intermediate 21 and 2-imidazol-1-ylbenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.81 (t, 1H), 7.53 (m, 1H), 7.5-7.42 (2m, 2H), 7.41 (t, 1H), 7.35 (m , 1H), 7.1 (t, 1H), 4.05-4 (m, 2H), 3.4 (dd, 2H), 3.3 (m, 2H), 2.9 / 2.4 (2m, 2H), 2.68 / 2.6 (2dd, 2H), 1.9-1.6 (m, 4H), 1.45 (s, 18H), 1.35 (m, 2H), 1.35 (s, 9H), 1.21 (t, 3H) , 1-0.65 (2m, 2H) EXAMPLE 98: 3-(4-Aminobutyl)-4-hydroxy-1-[(2-imidazol-1-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 98 is obtained from intermediate 86 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.9 (si, 1 H), 7.7-7.45 (m, 4 H), 7.36 (si, 1 H), 7.25 (si, 1 H), 4.25 (dd, 2 H), 3.5-3 (m, 4H), 2.95 (m, 2H), 2.1 / 1.7 (2m, 2H), 1.85 / 1.4 (2m, 2H), 1.6 (m, 2H), 1.15 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 407.1852 (407.1848) Elemental Analysis: C=56.41(56.15);H=5.89(6.70);N=13.55(13.79) Intermediate 87: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-piperazin-1-ylphenyl)methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 87 is obtained from intermediate 21 and 1-Boc-4(2-formylphenyl)piperazine according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.35 (dd, 1H), 7.24 (td, 1H), 7.11 (dd, 1H), 7.07 (td, 1H), 4.1-4 (m , 2H), 3.58 (dd, 2H), 3.46 (m, 4H), 3.3 (m, 2H), 2.9-2.5 (m, 8H), 1.9 (m, 2H), 1.75 (m , 2H), 1.4 (s, 18H), 1.4 (s, 9H), 1.35 (s, 9H), 1.35 (m, 2H), 1.25 (t, 3H), 0.85 (m, 2 H) EXAMPLE 99: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-piperazin-1-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 99 is obtained from intermediate 87 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.6-7.25 (m, 4H), 4.3 (dd, 2H), 3.75-3.05 (m, 12H), 2.9 (m, 2H), 2.2 / 1.75 (2m, 2H), 1.9 / 1.5 (2m, 2H), 1.6 (m, 2H), 1.3 / 1.15 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 425.2317 (425.231768) Elemental Analysis: C=47.64(47.53);H=6.01(6.78);N=11.07(11.09);Br-=15.70(15.81) Intermediate 88: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl} tert-Butyl-4-ethoxy-4-oxo-1-[[2-(2-oxo-1,3-oxazolidin-3-yl)phenyl]methyl]-1,4-azaphosphinane-3-carboxylate Intermediate 88 is obtained from intermediate 21 and 2-(2-oxooxazolidin-3-yl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.5-7.3 (m, 4H), 4.5 (t, 2H), 4.15-4 (m, 2H), 4-3.85 (2m, 2H) , 3.5 (dd, 2H), 3.35 (m, 2H), 2.9-2.5 (m, 4H), 2-1.7 (m, 4H), 1.42 (s, 18H), 1.4 (m, 2 H), 1.38 (s, 9H), 1.25 (t, 3H), 0.85 (m, 2H) EXAMPLE 100: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[2-(2-oxo-1,3-oxazolidin-3-yl)phenyl]methyl]-1,4-acid azaphosphinane-3-carboxylic Example 100 is obtained from intermediate 88 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.71-7.42 (m, 4H), 4.64 (t, 2H), 4.38 (s, 2H), 4.12 / 4.03 (m, 2H), 3.65 / 3.38 (dd, 2H), 3.46 / 3.16 (dd, 2H), 2.94 (t, 2H), 2.24 / 1.76 (m, 2H), 1.93 / 1.47 (m, 2H), 1.6 (t, 2 H), 1.26 / 1.12 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 426.1782 (426.1793) Elemental Analysis: C=53.51(53.64);H=6.34(6.63);N=9.71(9.88) Intermediate 89: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(3-methylimidazol-4-yl)phenyl]methyl]-4-oxo-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 89 is obtained from intermediate 21 and 3-(methylimidazol-4-yl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.7 (s, 1 H), 7.52 (dd, 1 H), 7.4 / 7.35 (2t, 2 H), 7.25 (dd, 1 H), 6.86 (s , 1H), 4.1-4 (m, 2H), 3.45-3.25 (m, 2H), 3.4 (s, 3H), 3.35 (m, 2H), 2.95 / 2.4 (2m, 2H), 2.85-2.6 (2m, 2H), 1.95-1.8 (m, 2H), 1.75 (m, 2H), 1.45 (s, 18H), 1.4 (m, 2H), 1.35 (s, 9H), 1.25 (t, 3H), 0.9-0.7 (2m, 2H) EXAMPLE 101: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(3-methylimidazol-4-yl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid L example 101 is obtained from intermediate 89 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.8 (s, 1H), 7.65 (m, 1H), 7.59 (m, 2H), 7.45 (m, 1H), 7.08 (d, 1H) , 4.24 (dl, 2H), 3.43 (s, 3H), 3.36 / 3.02 (dd, 2H), 3.19 (m, 2H), 2.94 (m, 2H), 2.15 / 1.73 (m, 2 H), 1.9 / 1.44 (m, 2H), 1.6 (m, 2H), 1.15 (dl, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 421.1999 (421.2004) Elemental Analysis: C=58.05(57.13);H=6.09(6.95);N=13.62(13.33) Intermediate 90: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(1-methylimidazol-2-yl)phenyl]methyl]-4-oxo- tert-Butyl 1,4-azaphosphinane-3-carboxylate Intermediate 90 is obtained from intermediates 21 and 223 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.55 (dd, 1H), 7.45 / 7.35 (2t, 2H), 7.31 (dd, 1H), 7.25 (d, 1H), 6.98 (d , 1H), 4 (m, 2H), 3.5 (dd, 2H), 3.48 (s, 3H), 3.4 (m, 2H), 2.95 / 2.35 (2m, 2H), 2.7-2.4 (2m, 2H), 1.85-1.75 (m, 2H), 1.7 (m, 2H), 1.45 (s, 18H), 1.4 (m, 2H), 1.35 (s, 9H), 1.2 (t, 3H), 0.85 (m, 2H) EXAMPLE 102: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(1-methylimidazol-2-yl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 102 is obtained from intermediate 90 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.7-7.5 (m, 4 H), 7.23 (d, 1 H), 7.16 (d, 1 H), 4.17 (dd, 2 H), 3.61 (s, 3 H), 3.46 / 3.26 (2m, 2H), 3.37 / 3.09 (dd, 2H), 2.8 (m, 2H), 2.11 / 1.83 (2m, 2H), 1.94 / 1.4 (2m, 2H) , 1.5 (m, 2H), 1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 421.2013 (421.2004) Elementary Analysis: C=57.28(57.13);H=7.10(6.95);N=13.21(13.33) Intermediate 91: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-fluoro-2-(4-methoxyphenyl)phenyl]methyl]-4-oxo- tert-Butyl 1,4-azaphosphinane-3-carboxylate Intermediate 91 is obtained from intermediates 21 and 221 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.48 (dd, 1H), 7.33 (d, 2H), 7.16 (td, 1H), 7.02 (dd, 1H), 7.02 (d, 2 H), 4.03 (m, 2H), 3.8 (s, 3H), 3.4 (AB, 2H), 3.32 (m, 2H), 2.66 / 2.51 / 2.41 (3m, 4H), 1.91-1.66 (m, 4H), 1.41 (s, 18H), 1.37 (m, 2H), 1.34 (s, 9H), 1.22 (t, 3H), 0.88 / 0.76 (2m, 2H) EXAMPLE 103: 3-(4-Aminobutyl)-1-[[4-fluoro-2-(4-methoxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 103 is obtained from intermediate 91 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.62 (dd, 1H), 7.35 (d, 2H), 7.24 (td, 1H), 7.17 (dd, 1H), 7.13 (d, 2H) , 4.36 (AB, 2H), 3.89 (s, 3H), 3.37 / 3.14 (2m, 2H), 3.14 / 2.85 (2m, 2H), 2.97 (m, 2H), 2.09 / 1.66 (2m , 2H), 1.88 / 1.38 (2m, 2H), 1.62 (m, 2H), 1.09 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 465.1965 (465.1954) Elemental Analysis: C=59.91(59.48);H=6.23(6.51);N=6.25(6.03) EXAMPLE 104: 3-(4-Aminobutyl)-1-[[4-fluoro-2-(4-hydroxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 104 is obtained from intermediate 91 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.62 (dd, 1H), 7.3 (d, 2H), 7.25 (td, 1H), 7.18 (dd, 1H), 7.03 (d, 2H) , 4.39 (AB, 2H), 3.4 / 3.13 (2m, 2H), 3.18 / 2.88 (2m, 2H), 2.99 (m, 2H), 2.12 / 1.68 (2m, 2H), 1.89 / 1.38 (2m, 2H), 1.63 (m, 2H), 1.12 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 451.1816 (451.1798) Elemental Analysis: C=58.99(58.66);H=6.33(6.27);N=6.27(6.22) Intermediate 92: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-phenylthiophen-3-yl)methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 92 is obtained from intermediates 21 and 224 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.55-7.34 (m, 5H), 7.55-7.34 (m, 1H), 7.09 (d, 1H), 4.04 (m, 2H), 3.51 (dd, 2H), 3.34 (m, 2H), 2.88-2.52 (m, 4H), 1.91 (m, 2H), 1.74 (m, 2H), 1.41 (s, 18H), 1.38 (m, 2H), 1.35 (s, 9H), 1.23 (t, 3H), 0.89 (m, 2H) EXAMPLE 105: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-phenylthiophen-3-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 105 is obtained from intermediate 92 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.52 (d, 1H), 7.4 (m, 5H), 7.2 (d, 1H), 4.4-4.25 (m, 2H), 3.6-3.4 (m , 1H), 3.2-3.1 (m, 2H), 2.9 (m, 2H), 2.7 (m, 1H), 2.15 (m, 1H), 1.85 (m, 1H), 1.65-1.5 (m, 3H), 1.3 (m, 1H), 1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 423.1511 (423.1507) Elemental Analysis: C=56.99(56.86);H=6.31(6.44);N=6.79(6.63);S=7.29(7.59) Intermediate 93: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}- tert-Butyl 4-ethoxy-4-oxo-1-[(4-phenylthiophen-3-yl)methyl]-1,4-azaphosphinane-3-carboxylate Intermediate 93 is obtained from intermediates 21 and 252 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.53 (d, 2H), 7.5 / 7.47 (2d, 2H), 7.41 (t, 2H), 7.33 (t, 1H), 4.04 (m , 2H), 3.47 (AB, 2H), 3.32 (m, 2H), 2.92-2.4 (m, 4H), 1.94-1.6 (m, 4H), 1.43 / 1.41 (2s, 18H) , 1.34 (2s, 9H), 1.33 (m, 2H), 1.22 (t, 3H), 0.8 (m, 2H) EXAMPLE 106: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(4-phenylthiophen-3-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 106 is obtained from intermediate 93 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.75 (d, 1H), 7.45 (m, 5H), 7.42 (d, 1H), 4.4-4.3 (2*d, 2H), 3.45 / 3.15 (m, 2H), 3.15 / 2.75 (m, 2H), 2.9 (m, 2H), 2.1 (m, 1H), 1.8 (m, 1H), 1.7-1.5 (m, 3H) , 1.25 (m, 1H), 0.95 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 423.1503 (423.1507) Elemental Analysis: C=57.35(56.86);H=6.30(6.44);N=6.53(6.63);S=7.56(7.59) Intermediate 94: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl }-4-ethoxy-4-oxo-l- tert-Butyl (thiophen-2-ylmethyl)-l,4-azaphosphinane-3-carboxylate Intermediate 94 is obtained from intermediate 21 and 2-formylthiophene according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.43 (m, 1H), 6.97 (m, 2H), 4.05 (m, 2H), 3.77 (AB, 2H), 3.41 (m, 2 H), 2.85 / 2.55 (2m, 2H), 2.85 / 2.66 (2m, 2H), 2-1.7 (m, 4H), 1.43 (s, 18H), 1.41 (m, 2H), 1.39 (s, 9H), 1.24 (t, 3H), 1.01 (m, 2H) EXAMPLE 107: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-(thiophen-2-ylmethyl)-1,4-azaphosphinane-3-carboxylic acid Example 107 is obtained from intermediary 94 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.6 (dl, 1H), 7.25 (dl, 1H), 7.12 (t, 1H), 4.6 / 4.5 (d, 2H), 3.75 / 3.3 (m , 2H), 3.6 / 3.12 (m, 2H), 2.95 (m, 2H), 2.25 / 1.8 (m, 2H), 1.95 / 1.5 (m, 2H), 1.6 (m, 2H) , 1.3-1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 347.1205 (347.1194) Elemental Analysis: C=48.94(48.55);H=5.79(6.69);N=7.90(8.09);S=9.22(9.26) Intermediate 95: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[[2-(1,3-thiazol-2-yl)phenyl]methyl tert-Butyl]-l,4-azaphosphinane-3-carboxylate Intermediate 95 is obtained from intermediates 21 and 225 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.98 (d, 1 H), 7.85 (d, 1 H), 7.7 (d, 1 H), 4.45 (m, 3 H), 4.05 (quad., 2H), 3.45 / 3.35 (d, 2H), 3.4 / 2.5 (m, 2H), 3.3 (m, 2H), 2.7 / 2.5 (m, 2H), 1.8- 1.55 (m, 4H ), 1.45-1.35 (m, 2H), 1.4 / 1.3 (s, 27H), 1.2 (t, 3H), 0.65-0.3 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 708.3453 (708.3447) EXAMPLE 108: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[2-(1, 3-thiazol-2-yl)phenyl]methyl]-1,4-azaphosphinane-3-carboxylic Example 108 is obtained from intermediate 95 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.98 (m, 2 H), 7.85 (m, 4 H), 4.6 (d, 1 H), 4.2 (d, 1 H), 3.85 (m, 1 H) , 3.45 (m, 2 hrs), 3.15 (dd, 1 hr), 2.9 (m, 2 hrs), 2.3 (m, 1 hrs), 1.85 (m, 2 hrs), 1.55 (m, 3 hrs), 1.2 (m, 1H), 1.0 (m, 1H) ESI / FIA / HR and MS / MS: [M+H]+ = 424.1443 (424.1459) Elemental Analysis: C=54.17(53.89);H=5.57(6.19);N=9.91(9.92);S=7.38(7.57) Intermediate 96: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(2-naphthalen-1-ylphenyl)methyl]-4-oxo-1,4-azaphosphinan-3 - tert-butyl carboxylate Intermediate 96 is obtained from intermediates 21 and 228 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8-7.15 (m, 1 1 H), 4.05-3.8 (m, 2 H), 3.5-3.3 (m, 2 H), 3.3-3 (dd, 2H), 2.7-2.1 (m, 4H), 2-1.5 (m, 4H), 1.5-1.3 (m, 2H), 1.45 (s, 18H), 1.35 (s, 9H), 1.2 (t, 3H), 1-0.5 (m, 2H) EXAMPLE 109: 3-(4-Aminobutyl)-4-hydroxy-1-[(2-naphthalen-1-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 109 is obtained from intermediate 96 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8 (d, 2 H), 7.75-7.3 (m, 9 H), 4.3 / 4.05 (2*d, 1 H), 3.95 / 3.8 (2*d, 1 H), 3.55-2.8 (m, 5H), 2.65 (m, 1H), 2.2-1.9 (m, 1H), 1.75 (m, 1H), 1.7-1.4 (m, 3H), 1.35 -0.7 (m, 3H) ESI / FIA / HR and MS / MS: [M+H]+ = 467.2109 (467.2099) Elemental Analysis: C=67.08(66.94);H=6.21(6.70);N=5.75(6.00) Intermediate 97: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(4-phenylthiophen-2-yl)methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 97 is obtained from intermediate 21 and 4-phenyl-2-thiophenecarboxaldehyde according to procedure F previously described. 1H NMR: (500 MHz, dmso-d6) δ ppm 7.75 (d, 1H), 7.67 (d, 2H), 7.41 (d, 1H), 7.39 (t, 2H), 7.27 (t, 1 H), 4.07 (m, 2H), 3.8 (AB, 2H), 3.4 (m, 2H), 2.95 / 2.58 (2m, 2H), 2.89 / 2.71 (2m, 2H), 2-1.74 (m, 4H), 1.43 / 1.4 / 1.39 / 1.37 (5s, 27H), 1.4 (m, 2H), 1.24 / 1.2 (2t, 3H), 1.1 / 1 (2m, 2H) EXAMPLE 110: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(4-phenylthiophen-2-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 110 is obtained from intermediate 97 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.75 (s, 1H), 7.65 (d, 2H), 7.6 (s, 1H), 7.42 (d, 2H), 7.3 (t, 1H) , 4.6 / 4.5 (2*d, 2H), 3.8-3.35 (m, 3H), 3.1 (m, 1H), 2.85 (m, 2H), 2.25 / 1.8 (m, 2H), 1.95 / 1.45 (m, 2H), 1.55 (m, 2H), 1.25-1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 423.151 (423.1507) Elemental Analysis: C=57.05(56.86);H=6.10(6.44);N=6.67(6.63);S=7.51(7.59) Intermediate 98: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[(2-bromo-4-hydroxyphenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 98 is obtained from intermediate 21 and 2-bromo-4-methoxybenzaldehyde according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.3 (d, 1H), 7.2 (s, 1H), 6.95 (dd, 1H), 4.05 (m, 2H), 3.75 (s, 3 H), 3.6-3.5 (d, 2H), 3.4-3.3 (m, 2H), 3-2.6 (m, 4H), 2.9-1.5 (m, 4H), 1.42 / 1.35 (s, 27 H), 1.4 (m, 2H), 1.22 (t, 3H), 0.75 (m, 2H) NMR 31 P: (300 MHz, dmso-d6) δ ppm 47.5 EXAMPLE 111: 3-(4-Aminobutyl)-1-[(2-bromo-4-hydroxyphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 111 is obtained from intermediate 98 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.38 (d, 1H), 7.2 (s, 1H), 6.9 (dd, 1H), 4.4-4.3 (2*d, 2H), 3.8-3.7 (m, 1H), 3.6-3.4 (m, 2H), 3.25 (dd, 1H), 2.95 (m, 2H), 2.25 (m, 1H), 1.95 (m, 1H), 1.8 (m, 1H), 1.65-1.5 (m, 3H), 1.3 (m, 1H), 1.15 (m, 1H) ESI / FIA / HR and MS / MS: [M+H]+ = 435.067 (435.0684) Elemental Analysis: C=44.16(44.15);H=5.06(5.56);N=6.05(6.44) Intermediate 99: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[[2-(4-chlorophenyl)pyridin-3-yl]methyl]-4-ethoxy-4-oxo-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 99 is obtained from intermediates 21 and 291 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.58 (m, 1H), 7.9 / 7.89 (2dd, 1H), 7.63 / 7.61 (2d, 2H), 7.53 (d, 2H), 7.4 (dd, 1H), 4.04 / 3.94 (2m, 2H), 3.56 / 3.53 (2AB, 2H), 3.32 (m, 2H), 2.76-2.25 (m, 4H), 1.95-1.65 (m , 4H), 1.43 / 1.41 (2s, 18H), 1.35 (m, 2H), 1.33 / 1.32 (2s, 9H), 1.23 / 1.18 (2t, 3H), 0.9 / 0.74 (2m, 2 H) EXAMPLE 112: 3-(4-Aminobutyl)-1-[[2-(4-chlorophenyl)pyridin-3-yl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan-3-acid carboxylic Example 112 is obtained from intermediate 99 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 8.61 (dd, 1 H), 8.09 (dd, 1 H), 7.56 / 7.43 (2d, 4 H), 7.55 (dd, 1 H), 4.42 (AB, 2 H), 3.45 / 3.1 (2m, 2H), 3.1 / 2.87 (2m, 2H), 2.9 (m, 2H), 2.1 / 1.65 (2m, 2H), 1.82 / 1.33 (2m, 2H) , 1.55 (m, 2H), 1.03 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 452.1508 (452.1505) Elemental Analysis: C=55.90(55.82);H=6.11(6.02);N=8.95(9.30) Intermediate 100: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[[4-chloro-2-(4-chlorophenyl)phenyl]methyl]-4-ethoxy-4-oxo-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 100 is obtained from intermediates 21 and 292 according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.55-7.35 (m, 6H), 7.25 (s, 1H), 4.15-4 (m, 2H), 3.5- 3.3 (m, 4H) , 2.95-2.4 (m, 4H), 1.95-1.6 (m, 6H), 1.5-1.3 (3t, 27H), 1.25 (t, 3H), 1.15-0.75 (m, 2H) EXAMPLE 113: 3-(4-Aminobutyl)-1-[[4-chloro-2-(4-chlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 113 is obtained from intermediate 100 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.58 (d, 1H), 7.54 (d, 2H), 7.54 (dd, 1H), 7.45 (d, 1H), 7.33 (d, 2H) , 4.33 (dd, 2H), 3.41 / 3.1 (2m, 2H), 3.15 / 2.85 (dd, 2H), 2.95 (m, 2H), 2.1 / 1.65 (2m, 2H), 1.85 / 1.35 (2m, 2H), 1.6 (m, 2H), 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 485.1172 (485.1163) Elemental Analysis: C=54.57(54.44);H=5.31(5.61);N=5.84(5.77) Intermediate 101: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[[2-(2-phenylphenyl)phenyl]methyl]-1,4- tert-butyl azaphosphinane-3-carboxylate Intermediate 101 is obtained from intermediates 21 and 238 according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.6-7 (m, 13 H), 4.15-3.9 (m, 2 H), 3.5-3.3 (m, 2 H), 3.3-2.9 (m, 2 H), 2.75-2.2 (m, 4H), 1.95-1.65 (m, 4H), 1.6-1.3 (m, 2H), 1.45 (3s, 27H), 1.25 (t, 3H), 1.2 -0.7 (m, 2H) EXAMPLE 114: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[2-(2-phenylphenyl)phenyl]methyl]-1,4-azaphosphinane-3-carboxylic acid Example 114 is obtained from intermediate 101 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.6-7.1 (m, 13 H), 3.8 / 3.6 / 3.55 (2*d, 2 H), 3.3 / 3 (2*m, 2 H), 3.15 / 2.6 (2*m, 2H), 2.92 (m, 2H), 2.05 / 1.6 (2*m, 2H), 1.8 / 1.3 (2*m, 2H), 1.6 (m, 2H), 1.02 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 493.2273 (493.2256) Elemental Analysis: C=68.12(68.28);H=6.31(6.75);N=5.77(5.69) Intermediate 102: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[[2-[3-(trifluoromethoxy)phenyl]phenyl]methyl]-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 102 is obtained from intermediate 21 and 2-[3-(trifluoromethoxyphenyl)]benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.59 (t, 1H), 7.42 (m, 3H), 7.42 (m, 3H), 7.28 (m, 1H), 3.99 (m, 2 H), 3.54 / 3.32 (m, 2H), 3.32 (m, 2H), 3.1-2.2 (m, 2H), 3.1-2.2 (m, 2H), 2-1.6 (m, 2H) , 2-1.6 (m, 2H), 1.5-1.3 (m, 27H), 1.3 (m, 2H), 1.21 (t, 3H), 0.9-0.5 (m, 2H) EXAMPLE 115: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[2-[3- (trifluoromethoxy)phenyl] phenyl] methyl]-1,4-azaphosphinane-3-carboxylic Example 115 is obtained from intermediate 102 according to procedure D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.63 (m, 1H), 7.59 (t, 1H), 7.55 (m, 2H), 7.41 (m, 1H), 7.41 (m, 1 H), 7.34 (m, 2H), 4.41 / 3.2 (2*d, 2H), 3.43 / 3.1 (m, 2H), 3.2 / 2.84 (m, 2H), 2.94 (m, 2H) , 2.11 / 1.64 (m, 2H), 1.86 / 1.36 (m, 2H), 1.59 (m, 2H), 1.13 / 1.06 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 501.1759 (501.1766) Elemental Analysis: C=54.63(55.20);H=5.24(5.64);N=5.43(5.60) Intermediate 103: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-fluoro-2-phenylphenyl)methyl]-4-oxo-1,4-azaphosphinan-3 tert-butyl-carboxylate Intermediate 103 is obtained from intermediates 21 and 257 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 22 / 2.7 (2*m, 2 H), 7.52 (dd, 1 H), 7.47 (t, 2 H), 7.4 (t, 1 H), 7.37 (d, 2H), 7.2 (dt, 1H), 7.04 (dd, 1H), 4-3.7 (m, 2H), 3.52 / 3.32 (2*d, 2H), 3.32 (m, 2 H), 2.7 / 2.32 (2*m, 2H), 1.95-1.72 (m, 2H), 1.95-1.72 (m, 2H), 1.41 / 1.35 (2*s, 27H), 1.38 (m , 2H), 1.17 (t, 3H), 0.8-0.6 (m, 2H) EXAMPLE 116: 3-(4-Aminobutyl)-1-[(4-fluoro-2-phenylphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 116 is obtained from intermediate 103 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.6 (dd, 1H), 7.49 (m, 3H), 7.34 (m, 2H), 7.22 (td, 1H), 7.15 (dd, 1H) , 4.31 (AB, 2H), 3.32 / 3.06 (2m, 2H), 3.16 / 2.8 (2m, 2H), 2.92 (m, 2H), 2.05 / 1.6 (2m, 2H), 1.82 / 1.33 (2m, 2h), 1.56 (m, 2h), 1.07 (m, 2h) NMR 19 F: (300 MHz, D20) δ ppm -111.5 ESI / FIA / HR and MS / MS: [M+H]+ = 435.1854 (435.1848) Elemental Analysis: C=60.79(60.82);H=6.07(6.50);N=6.19(6.45) Intermediate 104: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-hydroxy-2-phenylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3 tert-butyl carboxylate Intermediate 104 is obtained from intermediates 21 and 285 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.45-7.32 (m, 5H), 7.42 (d, 1H), 6.95 (dd, 1H), 6.74 (df, 1H), 3.92 (m , 2H), 3.77 (s, 3H), 3.46 / 3.27 (2*d, 2H), 3.34 (m, 2H), 2.75 / 2.15 (2*m, 2 H), 2.68 / 2.28 (2*m, 2H), 1.85-1.65 (m, 2H), 1.85-1.65 (m, 2H), 1.69 (m, 2H), 1.41 / 1.34 (2*s , 27H), 1.39 (m, 2H), 1.17 (t, 3H) EXAMPLE 117: 3-(4-Aminobutyl)-4-hydroxy-1-[(4-hydroxy-2-phenylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 117 is obtained from intermediate 104 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.5-7.25 (m, 5 H), 7.3 (d, 1 H), 6.92 (dd, 1 H), 6.82 (d, 1 H), 4.3 / 4.15 (2 *d, 2H), 3.3 / 3 (2*m, 2H), 3.15 / 2.72 (dd, 2H), 2.9 (m, 2H), 2 / 1.55 ​​(2*m, 2H), 1.8 / 1.55 ​​(2*m, 2H), 1.55 / 1.3 (2*m, 2H), 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 433.1888 (433.1892) Elemental Analysis: C=60.92(61.10);H=6.44(6.76);N=6.43(6.48) Intermediate 105: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(furan-2-yl)phenyl]methyl]-4-oxo-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 105 is obtained from intermediate 21 and 2-(2-furyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.77 (d, 1H), 7.62 (d, 1H), 7.41 (d, 1H), 7.37 / 7.31 (2*m, 2H), 6.77 (d, 1H), 6.61 (dd, 1H), 3.96 (m, 2H), 3.84 / 3.49 (2*d, 2H), 3.3-3.15 (m, 2H), 2.95 / 2.38 (2 *m, 2H), 2.77 / 2.45 (2*m, 2H), 2.05-1.6 (m, 2H), 2.05-1.6 (m, 2H), 1.4 / 1.32 (2*s, 27H) , 1.3-1.15 (m, 2H), 1.2 (t, 3H), 0.7-0.48 (4*m, 2H) EXAMPLE 118: 3-(4-Aminobutyl)-1-[[2-(furan-2-yl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 118 is obtained from intermediate 105 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.75 (d, 1H), 7.73 (s, 1H), 7.52 (t, 1H), 7.48 (d, 1H), 7.4 (t, 1H) , 6.88 (d, 1H), 6.63 (d, 1H), 4.63 / 4.33 (2*d, 2H), 3.82 / 3.5 (2*m, 2H), 3.48 / 3.18 (dd, 2H) , 2.9 (m, 2H), 2.26 / 1.8 (2*m, 2H), 1.9 / 1.48 (2*m, 2H), 1.6 (m, 2H), 1.2 / 1.05 (2*m, 2 h) ESI / FIA / HR and MS / MS: [M+H]+ = 407.1729 (407.1735) Elemental Analysis: C=59.18(59.11);H=6.65(6.70);N=6.86(6.89) Intermediate 106: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-thiophen-2-ylphenyl)methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 106 is obtained from intermediate 21 and 2-(2-thienyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.62 (dd, 1H), 7.46-7.33 (m, 4H), 7.23 (dd, 1H), 7.14 (dd, 1H), 4.03-3.88 (sts, 2 hrs), 3.65 / 3.42 (2*d, 2 hrs), 3.32-3.15 (sts, 2 hrs), 3-2.7 / 2.4 (2*sts, 2 hrs), 3-2.7 / 2.4 (2 *m, 2H), 2.05-1.75 (m, 2H), 2.05-1.75 (m, 2H), 1.4 / 1.34 (2*s, 27H), 1.39 (m, 2H), 1.2 (t , 3H), 0.7-0.45 (m, 2H) EXAMPLE 119: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-thiophen-2-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 119 is obtained from intermediate 106 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.6 (m, 1H), 7.57 (d, 1H), 7.52 (m, 2H), 7.52 (m, 1H), 7.2 (d, 1H) , 7.15 (d, 1H), 4.52 / 4.42 (2*d, 2H), 3.48 / 3.22 (2*m, 2H), 3.3 / 2.98 (dd, 2H), 2.93 (m, 2H) , 2.13 / 1.68 (2*m, 2H), 1.88 / 1.4 (2*m, 2H), 1.6 (m, 2H), 1.2 / 1.05 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 423.1493 (423.1507) Elemental Analysis: C=56.66(56.86);H=6.32(6.44);N=6.64(6.63);S=7.48(7.59) Intermediate 107: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-pyridin-4-ylphenyl)methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 107 is obtained from intermediates 21 and 258 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.62 (d, 2H), 7.5 (dd, 1H), 7.46-7.37 (m, 2H), 7.4 (d, 2H), 7.26 (dd , 1H), 3.92 (m, 2H), 3.58 / 3.38 (2*d, 2H), 3.3 (m, 2H), 2.82 / 2.22 (2*m, 2H), 2.68 / 2.37 (2*m, 2H), 1.85-1.65 (m, 2H), 1.85-1.65 (m, 2H), 1.41 / 1.33 (2*s, 27H), 1.38 (m, 2H), 1.18 (t, 3H), 0.63 (m, 2H) NMR 13 C: (400 MHz, dmso-d6) δ ppm 107, 67, 29 / 23 EXAMPLE 120: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-pyridin-4-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 120 is obtained from intermediate 107 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.59 (d, 2H), 7.62 (m, 1H), 7.55 (m, 2H), 7.41 (d, 2H), 7.41 (m, 1H) , 4.4 / 4.29 (2*d, 2H), 3.42 / 3.09 (2*m, 2H), 3.18 / 2.85 (2*m, 2H), 2.91 (m, 2H), 2.08 / 1.65 (2 *m, 2H), 1.82 / 1.55 ​​(2*m, 2H), 1.55 / 1.32 (2*m, 2H), 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 418.1891 (418.1895) Elemental Analysis: C=59.87(60.42);H=6.51(6.76);N=9.86(10.07) Intermediate 108: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-pyridin-3-ylphenyl)methyl]-1,4-azaphosphinan-3 tert-butyl-carboxylate Intermediate 108 is obtained from intermediate 21 and 2-(3-pyridyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.58 (dd, 1H), 8.56 (d, 1H), 7.81 (dt, 1H), 7.48 (m, 1H), 7.48 (m, 1 H), 7.41 (m, 2H), 7.27 (d, 1H), 3.93 (m, 2H), 3.55 / 3.35 (2*d, 2H), 3.29 (m, 2H), 2.71 / 2.2 (m, 2H), 2.71 / 2.35 (m, 2H), 1.95-1.7 (m, 2H), 1.95-1.7 (m, 2H), 1.41 (s, 18H), 1.36 (m, 2 H), 1.34 (s, 9H), 1.18 (t, 3H), 0.64 (m, 2H) EXAMPLE 121: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-pyridin-3-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 121 is obtained from intermediate 108 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.58 (dd, 1H), 8.51 (d, 1H), 7.86 (dt, 1H), 7.67 (m, 1H), 7.58 (m, 1H) , 7.58 (m, 2 hrs), 7.43 (m, 1 hrs), 4.42 / 4.3 (2*d, 2 hrs), 3.46 / 3.1 1 (m, 2 hrs), 3.2 / 2.87 (m, 2 hrs), 2.94 (m, 2H), 2.11 / 1.65 (m, 2H), 1.86 / 1.36 (m, 2H), 1.59 (m, 2H), 1.08 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 418.1898 (418.1895) Elemental Analysis: C=60.58(60.42);H=6.51(6.76);N=10.09(10.07) Intermediate 109: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[[2-[4-(trifluoroomethyl)phenyl]phenyl]methyl]- tert-Butyl 1,4-azaphosphinane-3-carboxylate Intermediate 109 is obtained from intermediate 21 and 2-[4-(trifluoromethyl)phenyl]benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.81 (d, 2H), 7.62 (d, 2H), 7.5 (d, 1H), 7.41 (m, 2H), 7.27 (d, 1 H), 3.93 (m, 2H), 3.58 / 3.34 (2*d, 2H), 3.28 (m, 2H), 2.74 / 2.36 (m, 2H), 2.74 / 2.24 (m, 2H) , 2-1.7 (m, 2 hrs), 2-1.7 (m, 2 hrs), 1.4 (s, 18 hrs), 1.36 (m, 2 hrs), 1.34 (s, 9 hrs), 1.17 (t, 3 H), 0.65 (m, 2H) EXAMPLE 122: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[2-[4- (Trifluor omethyl)phenyl] phenyl] methyl]-1,4-azaphosphinane-3-carboxylic Example 122 is obtained from intermediate 109 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.83 (d, 2H), 7.64 (m, 1H), 7.56 (m, 2H), 7.53 (d, 2H), 7.43 (m, 1H) , 4.42 / 4.28 (2*d, 2H), 3.42 / 3.09 (m, 2H), 3.18 / 2.84 (m, 2H), 2.94 (m, 2H), 2.1 / 1.64 (m, 2H) , 1.85 / 1.35 (m, 2H), 1.59 (m, 2H), 1.13 / 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 485.1800 (485.1817) Elemental Analysis: C=56.24(57.02);H=5.26(5.83);N=5.65(5.78) Intermediate 110: terf -butyl Intermediate 110 is obtained from intermediate 21 and 2-cyclohexylbenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.28 / 7.17 (2*d, 2 H), 7.22 / 7.1 (2*m, 2 H), 3.98 (m, 2 H), 3.5 (s, 2 H), 3.31 (m, 2H), 3-2.8 / 2.28 (2*m, 2H), 3-2.8 / 2.5 (2*m, 2H), 3-2.8 (m, 1H), 2 - 1.78 (2*m, 2H), 1.9-1.65 (m, 2H), 1.9-1.65 (m, 6H), 1.45-1.25 (m, 2H), 1.45-1.25 (m, 4H), 1.41 / 1.37 (2*s, 27H), 1.21 (t, 3H), 0.85-0.65 (m, 2H) EXAMPLE 123: 3-(4-Aminobutyl)-1-[(2-cyclohexylphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 123 is obtained from intermediary 110 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.52-7.4 (m, 2 H), 7.52-7.4 / 7.3 (2*m, 2 H), 4.4 (t, 2 H), 3.6 / 3.4 (2*m , 2H), 3.49 / 3.24 (2*m, 2H), 2.93 (m, 2H), 2.66 (m, 1H), 2.21 / 1.75 (2*m, 2H), 1.95 / 1.5 (2 *m, 2H), 1.85-1.1 (m, 10H), 1.85-1.1 (m, 4H) ESI / FIA / HR and MS / MS: [M+H]+ = 423.2408 (423.2412) Elemental Analysis: C=62.46(62.54);H=8.23(8.35);N=6.61(6.63) Intermediate 111: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-(1H-indazol-5-ylmethyl)-4-oxo-1,4-azaphosphinane-3- tert-butyl carboxylate Intermediate 111 is obtained from intermediate 21 and 1H-indazole-5-carbaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 13 (si, 1 H), 8 (s, 1 H), 7.62 (df, 1 H), 7.48 (d, 1 H), 7.3 (dd, 1 H), 3.97 (m, 2H), 3.72 / 3.52 (2*d, 2H), 3.4-3.2 (m, 2H), 2.96 / 2.32 (2*m, 2H), 2.83 / 2.47 (2 *m, 2H), 2-1.8 (m, 2H), 2-1.8 (m, 2H), 1.39 / 1.33 (2*s, 27H), 1.36 (m, 2H), 1.2 (t , 3 H), 0.9-0.7 (m, 2 H) EXAMPLE 124: 3-(4-Aminobutyl)-4-hydroxy-1-(1H-indazol-5-ylmethyl)-4-oxo-1,4-acid azaphosphinane-3-carboxylic Example 124 is obtained from intermediate 111 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.16 (s, 1 H), 7.91 (s, 1 H), 7.68 (d, 1 H), 7.49 (d, 1 H), 4.51 / 4.32 (2*d , 2H), 3.64 / 3.35 (2*m, 2H), 3.48 / 3.11 (2*m, 2H), 2.89 (m, 2H), 2.25 / 1.77 (2*m, 2H), 1.91 / 1.55 ​​(2*m, 2H), 1.55 / 1.45 (2*m, 2H), 1.19 / 1.05 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 381.1697 (381.1691) Elemental Analysis: C=53.27(53.68);H=6.55(6.62);N=14.52(14.73) Intermediate 112: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-thiophen-3-ylphenyl)methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 112 is obtained from intermediates 21 and 259 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.61 (dd, 1H), 7.59 (dd, 1H), 7.44 / 7.32 (2*m, 4H), 7.25 (dd, 1H), 3.95 (m, 2H), 3.6 / 3.4 (2*d, 2H), 3.3 (m, 2H), 2.8 / 2.29 (2*m, 2H), 2.8 / 2.4 (2*m, 2H) , 2-1.79 (m, 2 hrs), 2-1.79 (m, 2 hrs), 1.7 (m, 2 hrs), 1.4 / 1.34 (2*s, 27 hrs), 1.35 (m, 2 hrs), 1.19 (t, 3 H) EXAMPLE 125: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-thiophen-3-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 125 is obtained from intermediate 112 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.63-7.43 (m, 2H), 7.63-7.43 (m, 4H), 7.19 (dd, 1H), 4.49 / 4.34 (2*d, 2H) , 3.39 / 3.17 (2*m, 2H), 3.25 / 2.94 (2*m, 2H), 2.94 (m, 2H), 2.1 / 1.68 (2*m, 2H), 1.87 / 1.59 (2 *m, 2H), 1.59 / 1.39 (2*m, 2H), 1.18 / 1.05 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 423.1504 (423.1507) Elemental Analysis: C=57.17(56.86);H=6.48(6.44);N=6.67(6.63);S=7.11(7.59) Intermediate 113: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(3-fluorophenyl)phenyl]methyl]-4-oxo-1,4- tert-butyl azaphosphinane-3-carboxylate Intermediate 113 is obtained from intermediate 21 and 2-(3-fluorophenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.48 (m, 1H), 7.48 (m, 1H), 7.38 (m, 2H), 7.23 (m, 3H), 7.23 (m, 1 H), 3.93 (m, 2H), 3.56 / 3.36 (2*d, 2H), 3.29 (m, 2H), 2.73 / 2.36 (m, 2H), 2.73 / 2.23 (m, 2H) , 2-1.7 (m, 2 hrs), 2-1.7 (m, 2 hrs), 1.41 (s, 18 hrs), 1.36 (m, 2 hrs), 1.33 (s, 9 hrs), 1.17 (t, 3 H), 0.66 (m, 2H) EXAMPLE 126: 3-(4-Aminobutyl)-1-[[2-(3-fluorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 126 is obtained from intermediate 113 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.62 (m, 1H), 7.54 (m, 2H), 7.5 (m, 1H), 7.41 (m, 1H), 7.21 (m, 1H) , 7.16 (m, 1hr), 7.14 (m, 1hr), 4.44 / 4.31 (2*d, 2hrs), 3.43 / 3.11 (m, 2hrs), 3.21 / 2.86 (m, 2hrs), 2.94 (m, 2H), 2.1 1 / 1.64 (m, 2H), 1.86 / 1.36 (m, 2H), 1.59 (m, 2H), 1.09 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 435.1841 (435.1848) Elemental Analysis: C=61.58(60.82);H=5.84(6.50);N=6.51(6.45) Intermediate 114: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(5-phenyl-1,2-oxazol-4-yl)methyl] - tert-butyl 1,4-azaphosphinane-3-carboxylate Intermediate 114 is obtained from intermediates 21 and 219 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.6 (s, 1H), 7.9 (m, 2H), 7.55 (m, 3H), 4 (m, 2H), 3.6 (dd, 2 H), 3.3 (m, 2H), 3 / 2.35 (2m, 2H), 2.8 / 2.5 (2dd, 2H), 2 (m, 2H), 1.8 (m, 2H), 1.4 (s , 18H), 1.35 (s, 9H), 1.35 (m, 2H), 1.2 (t, 3H), 0.8 (m, 2H) EXAMPLE 127: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(5-phenyl-1,2-oxazol-4-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 127 is obtained from intermediate 114 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.66 (s, 1H), 7.75-7.55 (m, 5H), 4.5 (dd, 2H), 3.6 / 3.28 (2m, 2H), 3.2 / 2.9 (dd, 2H), 2.85 (m, 2H), 2.2 / 1.7 (2m, 2H), 1.85 / 1.25 (2m, 2H), 1.5 (m, 2H), 0.9 / 0.7 (2m, 2 h) ESI / FIA / HR and MS / MS: [M+H]+ = 408.1661 (408.1688) Intermediate 115: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[(5-bromo-2-phenylphenyl)methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3 - tert-butyl carboxylate Intermediate 115 is obtained from intermediate 21 and 5-bromo-2-phenylbenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.71 (df, 1H), 7.53 (dd, 1H), 7.45 (t, 2H), 7.4 (dd, 1H), 7.3 (d, 2 H), 7.16 (t, 1H), 3.92 (m, 2H), 3.58 / 3.35 (2*d, 2H), 3.4 (m, 2H), 2.74 / 2.22 (2*m, 2H) , 2.67 / 2.34 (2*m, 2H), 2-1.7 (m, 2H), 2-1.7 (m, 2H), 1.42 (m, 2H), 1.4 / 1.35 (2*s, 27 H), 1.17 (t, 3 H), 0.78 (m, 2 H) EXAMPLE 128: 3-(4-Aminobutyl)-1-[(5-bromo-2-phenylphenyl)methyl]-4-hydroxy-4-acid -oxo-1,4-azaphosphinane-3-carboxylic Example 128 is obtained from intermediate 115 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.81 (d, 1H), 7.7 (dd, 1H), 7.52 (t, 2H), 7.49 (t, 1H), 7.37 (d, 2H) , 7.31 (d, 1H), 4.4 / 4.28 (2*d, 2H), 3.32 / 2.88 (2*m, 2H), 3.2 / 3.1 (2*m, 2H), 2.95 (m, 2 H), 2.08 / 1.67 (2*m, 2H), 1.88 / 1.6 (2*m, 2H), 1.6 / 1.37 (2*m, 2H), 1.17 / 1.08 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 495.1041 (495.1048) Elemental Analysis: C=53.71(53.34);H=5.72(5.70);N=5.89(5.66) Intermediate 116: 3-{4-[Bis(tei"i-butoxtcarbonyl)amino]butyl}-4-ethoxy-4 -oxo-l-[[2-[4- tert-Butyl (trifluor omethoxy)phenyl] phenyl] methyl]-1,4-azaphosphinane-3-carboxylate Intermediate 116 is obtained from intermediates 21 and 286 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.65-7.33 (m, 4H), 7.65-7.33 (m, 3H), 7.25 (dd, 1H), 3.94 (m, 2H), 3.57 / 3.3 (2*d, 2H), 3.3 (m, 2H), 2.72 / 2.23 (2*m, 2H), 2.72 / 2.37 (2*m, 2H), 2-1.7 (m, 2 H), 2-1.7 (m, 2H), 1.4 / 1.34 (2*s, 24H), 1.35 (m, 2H), 1.17 (t, 3H), 0.65 (m, 2H) EXAMPLE 129: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[2-[4- (trifluor omethoxy)phenyl] phenyl] methyl]-1,4-azaphosphinane-3-carboxylic Example 129 is obtained from intermediate 116 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.62 (m, 1 H), 7.54 (m, 2 H), 7.44 (s, 4 H), 7.4 (m, 1 H), 4.42 / 4.28 (2*d , 2H), 3.4 / 3.12 (2*m, 2H), 3.2 / 2.88 (2*m, 2H), 2.94 (m, 2H), 2.1 / 1.64 (2*m, 2H), 1.86 / 1.59 (2*m, 2H), 1.59 / 1.38 (2*m, 2H), 1.15 / 1.05 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 501.1773 (501.1766) Elemental Analysis: C=55.71(55.20);H=5.27(5.64);N=5.62(5.60) Intermediate 117: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-fluoro-2-(4-fluorophenyl)phenyl]methyl]-4-oxo-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 117 is obtained from intermediates 21 and 271 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.49 (dd, 1H), 7.42 (dd, 2H), 7.29 (t, 2H), 7.21 (dt, 1H), 7.06 (dd, 1 H), 3.93 (m, 2H), 3.49 / 3.3 (2*d, 2H), 3.3 (m, 2H), 2.72 / 2.21 (2*m, 2H), 2.69 / 2.34 (2*m , 2H), 1.95-1.7 (massive, 2H), 1.95-1.7 (massive, 2H), 1.68 (m, 2H), 1.41 / 1.33 (2*s, 27H), 1.38 (m, 2 H), 1.18 (t, 3 H) EXAMPLE 130: 3-(4-Aminobutyl)-1-[[4-fluoro-2-(4-fluorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-acid 1,4-azaphosphinane-3-carboxylic Example 130 is obtained from intermediate 117 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.66 (dd, 1H), 7.38 (dd, 2H), 7.27 (t, 2H), 7.25 (df, 1H), 7.18 (dd, 1H) , 4.39 / 4.28 (2*d, 2H), 3.38 / 3.09 (2*m, 2H), 3.18 / 2.87 (2*m, 2H), 2.95 (m, 2H), 2.09 / 1.68 (2 *m, 2H), 1.86 / 1.6 (2*m, 2H), 1.6 / 1.37 (2*m, 2H), 1.15 / 1.07 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 453.1741 (453.1754) Elemental Analysis: C=58.67(58.40);H=5.99(6.01);N=6.46(6.19) Intermediate 118: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-1-[[2-[4-chloro-3-(trifluoromethyl)phenyl]phenyl]methyl]-4-ethoxy- tert-Butyl 4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 118 is obtained from intermediates 21 and 278 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.9 (d, 1H), 7.81 (d, 1H), 7.75 (dd, 1H), 7.42 / 7.32 (2m, 3H), 3.95 (m , 2H), 3.41 (AB, 2H), 3.2 (m, 2H), 2.79 / 2.37 (2m, 2H), 2.69 / 2.27 (2m, 2H), 1.95 / 1.7 (2m, 2H) , 1.8 / 1.7 (2m, 2H), 1.39 (s, 18H), 1.33 (s, 9H), 1.27 (m, 2H), 1.19 (t, 3H), 0.61 / 0.48 (2m, 2 H) EXAMPLE 131: 3-(4-Aminobutyl)-1-[[2-[4-chloro-3- (trifluoromethyl)phenyl]phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic Example 131 is obtained from intermediate 118 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.76 (si, 1H), 7.71 (d, 1H), 7.63 (m, 1H), 7.54 (dl, 1H), 7.54 (m, 2H) , 7.38 (m, 1H), 4.31 (AB, 2H), 3.46 / 3.08 (2m, 2H), 3.13 / 2.83 (2m, 2H), 2.92 (m, 2H), 2.11 / 1.64 (2m , 2H), 1.83 / 1.34 (2m, 2H), 1.57 (m, 2H), 1.06 (m, 2H) NMR 19 F: (300 MHz, D20) δ ppm -62.3 ESI / FIA / HR and MS / MS: [M+H]+ = 519.1442 (519.1427) Elemental Analysis: C=53.40(53.24);H=4.76(5.24);N=5.43(5.40) Intermediate 119: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[[2-(3-chlorophenyl)phenyl]methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 119 is obtained from intermediates 21 and 213 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.52 (t, 1 H), 7.45 (m, 3 H), 7.4 / 7.37 (2td, 2 H), 7.33 (dt, 1 H), 7.25 (dd , 1H), 3.94 (m, 2H), 3.53 / 3.32 (AB, 2H), 3.25 (m, 2H), 2.76 / 2.37 (2m, 2H), 2.7 / 2.25 (2m, 2H) , 1.95 / 1.78 (2m, 2H), 1.82 / 1.75 (2m, 2H), 1.41 (s, 18H), 1.33 (s, 9H), 1.33 (m, 2H), 1.18 (t, 3 H), 0.66 / 0.57 (2m, 2H) EXAMPLE 132: 3-(4-Aminobutyl)-1-[[2-(3-chlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 132 is obtained from intermediate 119 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.6 (m, 1H), 7.52 (m, 2H), 7.5-7.35 (m, 4H), 7.26 (m, 1H), 4.33 (AB, 2 H), 3.41 / 3.09 (2m, 2H), 3.16 / 2.81 (2m, 2H), 2.92 (m, 2H), 2.09 / 1.64 (2m, 2H), 1.83 / 1.34 (2m, 2H) , 1.56 (m, 2H), 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 451.1556 (451.1553) Elemental Analysis: C=58.91(58.60);H=5.83(6.26);N=6.32(6.21) Intermediate 120: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-l tert-Butyl -[[2-(4-methylphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 120 is obtained from intermediates 21 and 288 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.49 (dd, 1H), 7.33 (2*m, 2H), 7.23 (2*d, 4H), 7.18 (dd, 1H), 3.92 (m, 2H), 3.54 / 3.35 (2*d, 2H), 3.3 (m, 2H), 2.74 / 2.2 (2*m, 2H), 2.74 / 2.32 (2*m, 2H) , 2.36 (s, 3H), 1.95-1.75 (m, 2H), 1.95-1.75 (m, 2H), 1.41 / 1.33 (2*s, 27H), 1.38 (m, 2H), 1.17 (t, 3H), 0.71 (m, 2H) EXAMPLE 133: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(4-methylphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 133 is obtained from intermediate 120 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.6 (dd, 1 H), 7.52 / 7.5 (2*m, 2 H), 7.39 (dd, 1 H), 7.35 (d, 2 H), 7.25 (d , 2H), 4.43 / 4.28 (2*d, 2H), 3.36 / 3.1 (2*dd, 2H), 3.22 / 2.83 (2*dd, 2H), 2.94 (m, 2H), 2.38 (s, 3H), 2.09 / 1.64 (2*m, 2H), 1.86 / 1.6 (2*m, 2H), 1.6 / 1.35 (2*m, 2H), 1.15 / 1.05 (2*m , 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 431.2103 (431.2099) Elemental Analysis: C=64.12(64.17);H=7.45(7.26);N=6.50(6.51) Intermediate 121: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[[2-(2,4-dichlorophenyl)phenyl]methyl]-4-ethoxy-4-oxo-1,4- tert-butyl azaphosphinane-3-carboxylate Intermediate 121 is obtained from intermediates 21 and 251 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.73 (m, 1H), 7.51 (m, 1H), 7.51 (m, 1H), 7.42 / 7.35 (m, 2H), 7.31 (m , 1H), 7.12 (m, 1H), 3.92 (m, 2H), 3.5-3.2 (m, 2H), 3.5-3.2 (m, 2H), 2.68 / 2.12 (m, 2H) , 2.68 / 2.35 (m, 2H), 1.81 (m, 2H), 1.81 (m, 2H), 1.42 (2*s, 18H), 1.38 (m, 2H), 1.35 (2*s , 9 H), 1.17 (2*t, 3 H), 0.74 (m, 2 H) EXAMPLE 134: 3-(4-Aminobutyl)-1-[[2-(2,4-dichlorophenyl)phenyl]methyl acid ]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 134 is obtained from intermediate 121 according to procedure D previously described. 1H NMR: (400 / 500 MHz, D20) δ ppm 7.7-7.63 (m, 2H), 7.6-7.5 (m, 2H), 7.46 (dd, 1H), 7.33 (m, 1H), 7.3 / 7.28 (2*d, 1H), 4.42 / 4.19 / 3.99 (m, 2H), 3.64 / 3.41 / 3.14 (m, 2H), 3.38 / 3.12 / 2.99 / 2.84 (m, 2H), 2.95 (m, 2H), 2.14 / 1.67 (m, 2H), 1.9 / 1.4 (m, 2H), 1.58 (m, 2H), 1.19 / 1.11 (m, 2H) NMR 13C: (400 / 500 MHz, D20) δ ppm 132.1, 130.6, 129.5, 127.3, 57, 57, 51.8, 38.6, 27, 26.4, 24.5, 20 ESI / FIA / HR and MS / MS: [M+H]+ = 485.1166 (485.1163) Elemental Analysis: C=54.26(54.44);H=5.33(5.61);N=5.83(5.77) Intermediate 122: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(2-methoxyphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 122 is obtained from intermediates 21 and 282 according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.5 (d, 1H), 7.4-7.2 (m, 2H), 7.4-7.2 (m, 1H), 7.09 (m, 1H), 7.09 (m, 2H), 7.01 (t, 1H), 3.96 (m, 2H), 3.7 (s, 3H), 3.42 (m, 2H), 3.34 (dd, 2 H), 2.73 / 2.23 (m, 2H), 2.73 / 2.46 (m, 2H), 2-1.7 (m, 2H), 2-1.7 (m, 2H), 1.47 (s, 18H) , 1.42 (m, 2H), 1.4 (s, 9H), 1.21 (t, 3H), 0.96 (m, 2H) EXAMPLE 135: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(2-methoxyphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 135 is obtained from intermediate 122 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.7-7.1 (m, 4H), 7.7-7.1 (m, 4H), 4.4-3.9 (m, 2H), 3.74 (s, 3H), 3.7 -3 (m, 2H), 3.25-2.65 (m, 2H), 2.94 (m, 2H), 2.3-1.3 (m, 2H), 2.3-1.3 (m, 2H), 1.61 (m , 2H), 1.3-0.9 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 447.2031 (447.2048) Elemental Analysis: C=62.34(61.87);H=6.65(7.00);N=6.46(6.27) Intermediate 123: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(3-methoxyphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 123 is obtained from intermediates 21 and 281 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.49 (d, 1H), 7.35 (m, 2H), 7.35 (m, 1H), 7.21 (d, 1H), 6.95 (dd, 1 H), 6.89 (d, 1H), 6.86 (si, 1H), 3.93 (m, 2H), 3.79 (s, 3H), 3.55 / 3.37 (2*d, 2H), 3.29 (m , 2H), 2.74 / 2.21 (m, 2H), 2.74 / 2.33 (m, 2H), 2-1.7 (m, 2H), 2-1.7 (m, 2H), 1.41 (s, 18 H), 1.37 (m, 2H), 1.33 (s, 9H), 1.17 (t, 3H), 0.68 (m, 2H) EXAMPLE 136: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(3-methoxyphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 136 is obtained from intermediate 123 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.6 (m, 1H), 7.53 (m, 2H), 7.46 (t, 1H), 7.4 (m, 1H), 7.07 (dd, 1H) , 6.95 (m, 2H), 4.43 / 4.28 (2*d, 2H), 3.84 (s, 3H), 3.38 / 3.1 (m, 2H), 3.2 / 2.85 (m, 2H), 2.94 (m, 2H), 2.1 / 1.64 (m, 2H), 1.86 / 1.36 (m, 2H), 1.59 (m, 2H), 1.13 / 1.06 (m, 2 h) ESI / FIA / HR and MS / MS: [M+H]+ = 447.2064 (447.2048) Elemental Analysis: C=61.90(61.87);H=6.25(7.00);N=6.35(6.27) Intermediate 124: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4 tert-Butyl -oxo-1-[[2-(4-propan-2-ylphenyl)phenyl]methyl]-1,4-azaphosphinane-3-carboxylate Intermediate 124 is obtained from intermediates 21 and 289 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.49 (dd, 1H), 7.33 (2*m, 2H), 7.31 (d, 2H), 7.27 (d, 2H), 7.21 (dd , 1 H), 3.93 (m, 2 H), 3.6 / 3.35 (2*d, 2 H), 3.33 (m, 2 H), 2.95 (hept., 1 H), 2.73 / 2.23 (2*m, 2H), 2.73 / 2.34 (2*m, 2H), 1.9-1.75 (m, 2H), 1.9-1.75 (m, 2H), 1.41 / 1.32 (2*s, 27H), 1.38 ( m, 2H), 1.25 (d, 6H), 1.18 (t, 3H), 0.7 (m, 2H) EXAMPLE 137: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[2-(4-propan-2-ylphenyl)phenyl]methyl]-1,4-azaphosphinane-3-carboxylic acid Example 137 is obtained from intermediate 124 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.61 (dd, 1 H), 7.52 (2*t, 2 H), 7.43 (d, 2 H), 7.38 (dd, 1 H), 7.29 (d, 2 H), 4.42 / 4.24 (2*d, 2H), 3.35 / 3.1 1 (2*m, 2H), 3.22 / 2.83 (2*m, 2H), 2.97 (m, 1H), 2.95 ( m, 2H), 2.09 / 1.67 (2*m, 2H), 1.85 / 1.6 (2*m, 2H), 1.6 / 1.35 (2*m, 2H), 1.24 (d, 6H), 1.15 / 1.05 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 459.2418 (459.2412) Elemental Analysis: C=65.54(65.49);H=7.39(7.69);N=6.12(6.11) Intermediate 125: 3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-(1H-indazol-4-ylmethyl)-4-oxo-1,4-azaphosphinane-3- tert-butyl carboxylate Intermediate 125 is obtained from intermediate 21 and 1H-indazole-4-carbaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 13.01 (s, 1H), 8.19 (s, 1H), 7.44 (d, 1H), 7.27 (dd, 1H), 6.99 (d, 1 H), 3.98 (m, 2H), 3.93 / 3.71 (2*d, 2H), 3.29 / 3.16 (m, 2H), 3.03 / 2.37 (m, 2H), 2.83 / 2.52 (m, 2 H), 2-1.7 (m, 2H), 2-1.7 (m, 2H), 1.38 (s, 18H), 1.33 (s, 9H), 1.24 / 1.1 (m, 2H), 1.21 (t, 3 H), 0.65 / 0.51 (m, 2 H) EXAMPLE 138: 3-(4-Aminobutyl)-4-hydroxy-1-(1H-indazol-4-ylmethyl)-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 138 is obtained from intermediate 125 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 8.29 (s, 1H), 7.71 (dl, 1H), 7.49 (dd, 1H), 7.3 (dl, 1H), 4.65 (AB, 2H) , 3.71 / 3.39 (2m, 2H), 3.56 / 3.21 (2m, 2H), 2.87 (m, 2H), 2.19 / 1.74 (2m, 2H), 1.91 / 1.45 (2m, 2H), 1.54 (quint., 2 H), 1.08 (m, 2 H) ESI / FIA / HR and MS / MS: [M+H]+ = 381.1707 (381.1691) Elemental Analysis: C=53.52(53.68);H=6.73(6.62);N=14.77(14.73) Intermediate 126: 3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-[[3-(4-chlorophenyl)pyridin-4-yl]methyl]-4-ethoxy-4-oxo-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 126 is obtained from intermediate 21 and 3-(4-chlorophenyl)pyridine-4-carbaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.57 (d, 1H), 8.42 (s, 1H), 7.56 (d, 2H), 7.54 (d, 1H), 7.44 (d, 2 H), 3.94 (m, 2H), 3.53 (AB, 2H), 3.36 (m, 2H), 2.7 / 2.45 (2m, 2H), 2.7 / 2.26 (2m, 2H), 1.89 (m , 4H), 1.41 (s, 18H), 1.41 (m, 2H), 1.35 (s, 9H), 1.17 (t, 3H), 0.78 (m, 2H) EXAMPLE 139: 3-(4-Aminobutyl)-1-[[3-(4-chlorophenyl)pyridin-4-yl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid L example 139 is obtained from intermediate 126 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.62 (d, 1H), 8.54 (s, 1H), 7.67 (d, 1H), 7.58 (d, 2H), 7.38 (d, 2H) , 4.46 / 4.35 (2*d, 2H), 3.47 / 3.12 (2*m, 2H), 3.17 / 2.95 (2*m, 2H), 2.95 (m, 2H), 2.15 / 1.68 (2 *m, 2H), 1.87 / 1.61 (2*m, 2H), 1.59 / 1.38 (2*m, 2H), 1.08 (m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 25.1 NMR 13 C: (400 MHz, D20) δ ppm 147.4, 146.1, 128.3, 126.4, 122.2, 55, 53.2, 49.9, 36, 24.3, 23.9, 22.1, 17.3 ESI / FIA / HR and MS / MS: [M+H]+ = 452.1516 (452.1505) Elemental Analysis: C=55.97(55.82);H=5.86(6.02);N=9.28(9.30) Intermediate 127: 3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(3-phenyl-1-benzothiophen-2-yl)methyl]-1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 127 is obtained from intermediates 21 and 283 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.95 (m, 1H), 7.55 (t, 2H), 7.47 (t, 1H), 7.45-7.3 (m, 3H), 7.45-7.3 (m, 2H), 4.05 (m, 2H), 3.81 (dd, 2H), 3.42 / 3.33 (m, 2H), 2.88 / 2.53 (m, 2H), 2.88 / 2.7 (m, 2 H), 2-1.7 (m, 2H), 2-1.7 (m, 2H), 1.49 (m, 2H), 1.39 (s, 27H), 1.23 (t, 3H), 1.14 / 1.02 (m, 2 H) EXAMPLE 140: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(3-phenyl-1-benzothiophen-2-yl)methyl]-1,4-azaphosphinane acid -3-carboxylic Example 140 is obtained from intermediate 127 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.97 (d, 1H), 7.56 (m, 3H), 7.49 (d, 1H), 7.45 (t, 1H), 7.35 (m, 1H) , 7.35 (m, 2 hrs), 4.6 / 4.51 (dd, 2 hrs), 3.55 / 3.18 (m, 2 hrs), 3.26 / 2.9 (m, 2 hrs), 2.9 (m, 2 hrs), 2.18 / 1.68 (m, 2H), 1.86 / 1.34 (m, 2H), 1.56 (m, 2H), 1.04 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 473.1669 (473.1663) Elemental Analysis: C=61.52(61.00);H=5.76(6.19);N=5.51(5.93);S=6.56(6.79) EXAMPLE 141: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(3-phenylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 141 is obtained from intermediate 21 and 3-phenylbenzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.79-7.4 (m, 9 H), 4.49 (m, 1 H), 4.29 (d, 1 H), 3.76 (m, 1 H), 3.51 (dd, 1 H), 3.39 (m, 1H), 3.13 (dd, 1H), 2.89 (m, 2H), 2.27 (m, 1H), 1.92 (m, 1H), 1.79 (m, 1H) , 1.58 (massive, 2H), 1.48 (m, 1H), 1.21 (m, 1H), 1.09 (m, 1H) ESI / FIA / HR and MS / MS: [M+H]+ = 417.1937 (417.1943) Elemental Analysis: C=64.07(63.45);H=6.72(7.02);N=6.86(6.73) EXAMPLE 142: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-(4-phenylbutyl)-1,4-azaphosphinane-3-carboxylic acid Example 142 is obtained from intermediate 21 and 4-phenylbutanal according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.29 (t, 2 H), 7.21 (d, 2 H), 7.19 (t, 1 H), 3.5 (m, 1 H), 3.41 (dd, 1 H) , 3.2 (m, 1H), 3.07 (m, 2H), 3 (m, 1H), 2.92 (m, 2H), 2.61 (m, 2H), 2.19 (m, 1H), 1.9 (m, 1H), 1.75-1.1 (m, 10H) ESI / FIA / HR and MS / MS: [M+H]+ = 383.2092 (383.2099) Elemental Analysis: C=59.51(59.67);H=8.12(8.17);N=7.34(7.33) EXAMPLE 143: 3-(4-aminobutyl)-4-hydroxy-4-oxo-1-(5-phenylpentyl) acid -l,4-azaphosphinane-3-carboxylic acid Example 143 is obtained from intermediate 21 and 5-phenylpentanal according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.33 (t, 2 H), 7.26 (d, 1 H), 7.21 (t, 1 H), 3.6 (m, 1 H), 3.52 (dd, 1 H) , 3.28 (m, 1H), 3.1 (m, 3H), 2.99 (m, 2H), 2.62 (t, 2H), 2.22 (m, 1H), 1.98 (m, 1H), 1.8 -1.6 (massive, 2H), 1.8-1.15 (m, 10H) ESI / FIA / HR and MS / MS: [M+H]+ = 397.2251 (397.2256) Elemental Analysis: C=61.01(60.59);H=7.98(8.39);N=7.12(7.07) EXAMPLE 145: 3-(4-Aminobutyl)-4-hydroxy-1-[(4-methylsulfanylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 145 is obtained from intermediate 21 and 4-formylthioanisole according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.41 / 7.37 (2*d, 4H), 4.38 / 4.17 (2*d, 2H), 3.7 / 3.31 (2*m, 2H), 3.45 / 3.09 (2*m, 2H), 2.92 (m, 2H), 2.49 (s, 3H), 2.22 / 1.78 (2*m, 2H), 1.92 / 1.59 (2*m, 2H), 1.58 / 1.47 (2*m, 2H), 1.22 / 1.1 (2*m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 25.9 ESI / FIA / HR and MS / MS: [M+H]+ = 387.1512 (387.1507) Elemental Analysis: C=52.52(52.84);H=6.70(7.04);N=7.35(7.25);S=8.34(8.30) EXAMPLE 146: 3-(4-Aminobutyl)-1-[(3-carboxyphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 146 is obtained from intermediate 21 and methyl 3-formylbenzoate according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.03 (2*m, 2 H), 7.7 (d, 1 H), 7.59 (t, 1 H), 4.52 / 4.3 (2*d, 2H), 3.75 / 3.4 (2*m, 2H), 3.4 / 3.12 (2*m, 2H), 2.9 (m, 2H), 2.25 / 1.81 (2*m, 2H), 1.95 / 1.58 (2*m, 2H), 1.62-1.43 (solid, 2H), 1.2 / 1.1 (2*m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 25 ESI / FIA / HR and MS / MS: [M+H]+ = 385.1522 (385.1528) Elemental Analysis: C=53.60(53.12);H=6.54(6.56);N=7.42(7.29) EXAMPLE 147: 3-(4-Aminobutyl)-1-[(4-carboxyphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 147 is obtained from intermediate 21 and methyl 4-formylbenzoate according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 8 (d, 2 H), 7.6 (d, 2 H), 4.52 / 4.3 (2*d, 2 H), 3.75 / 3.4 (2*m, 2 H) , 3.45 / 3.13 (dd, 2 hrs), 2.9 (m, 2 hrs), 2.28 / 1.8 (2*m, 2 hrs), 1.9 / 1.55 ​​(2*m, 2 hrs), 1.55 / 1.5 (m, 2 H), 1.2 / 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 385.1524 (385.1528) Elemental Analysis: C=52.66(53.12);H=6.04(6.56);N=7.33(7.29) EXAMPLE 148: 3-(4-Aminobutyl)-1-[[4-(difluoromethoxy)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 148 is obtained from intermediate 21 and 4-(difluoromethoxy)benzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.5 (d, 2 H), 7.25 (d, 2 H), 6.83 (t, 1 H), 4.4 / 4.22 (2*d, 2 H), 3.7 / 3.32 (dd, 2H), 3.45 / 3.1 (dd, 2H), 2.92 (m, 2H), 2.25 / 1.78 (2*m, 2H), 1.9 / 1.6 (2*m, 2H), 1.6 / 1.46 (2*m, 2H), 1.22 / 1.1 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 407.1551 (407.1547) Elemental Analysis: C=50.33(50.25);H=5.97(6.20);N=7.02(6.89) EXAMPLE 149: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(1S)-1-phenylethyl]-1,4-azaphosphinane-3-carboxylic acid Example 149 is obtained from intermediate 21 and acetophenone according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.5 (m, 5 H), 4.67 (quad., 1 H), 3.72 / 3.53 (2*m, 1 H), 3.62 / 3.41 (2*m, 1 H ), 3.29 / 3.13 (2*m, 1H), 3.09-2.9 (m, 1H), 3.09-2.9 (m, 2H), 2.28 / 2.1 1 (2*m, 1H), 2-1.65 (m, 1H), 2-1.65 (m, 2H), 1.7 (2*d, 3H), 1.7-1.05 (m, 2H), 1.7-1.05 (m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 26.4 / 26.2 ESI / FIA / HR and MS / MS: [M+H]+ = 355.1807 (355.1781) Elemental Analysis: C=57.43(57.62);H=7.57(7.68);N=7.96(7.90) EXAMPLE 150: 3-(4-Aminobutyl)-1-[(3,4-difluorophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 150 is obtained from intermediate 21 and 3,4-difluorobenzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.46-7.22 (m, 3H), 4.28 (AB, 2H), 3.69 / 3.42 (2m, 2H), 3.34 / 3.1 (m+dd, 2H) , 2.92 (m, 2 hrs), 2.23 / 1.77 (2m, 2 hrs), 1.92 / 1.46 (2m, 2 hrs), 1.59 (quint., 2 hrs), 1.22 / 1.09 (2m, 2 hrs) NMR 19 F: (300 MHz, D20) δ ppm -135.5 NMR 31 P: (300 MHz, D20) δ ppm 23 ESI / FIA / HR and MS / MS: [M+H]+ = 377.1416 (377.1441) Elemental Analysis: C=50.40(51.06);H=6.20(6.16);N=7.38(7.44) EXAMPLE 151: 3-(4-Aminobutyl)-1-[[3-[(dimethylamino)methyl]-4-hydroxyphenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 151 is obtained from intermediate 21 and 3-(dimethylaminomethyl)-4-hydroxy-benzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.45 (d, 1H), 7.43 (s, 1H), 7.02 (d, 1H), 4.35 / 4.18 (2*d, 2H), 4.32 / 4.28 (2*d, 2H), 3.7 / 3.3 (2*m, 2H), 3.44 / 3.08 (dd, 2H), 2.9 (m, 2H), 2.8 (d, 6H), 2.2 / 1.75 (2*m, 2H), 1.9 / 1.45 (2*m, 2H), 1.6 (m, 2H), 1.25 / 1.1 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 414.2155 (414.2157) Elemental Analysis: C=46.97(47.82);H=5.90(6.31);N=7.67(7.97) EXAMPLE 152: 3-(4-Aminobutyl)-1-[(2-fluorophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 152 is obtained from intermediate 21 and 2-fluorobenzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.5 (m, 2 H), 7.26 (m, 2 H), 4.41 (si, 2 H), 3.7 / 3.35 (2m, 2 H), 3.52 / 3.21 (2m , 2 hrs), 2.94 (m, 2 hrs), 2.22 / 1.77 (2m, 2 hrs), 1.95 / 1.49 (2m, 2 hrs), 1.61 (quint., 2 hrs), 1.28 / 1.14 (2m, 2 hrs ) NMR 19 F: (300 MHz, D20) δ ppm -115 NMR 31 P: (300 MHz, D20) δ ppm 25.6 ESI / FIA / HR and MS / MS: [M+H]+ = 359.1530 (359.1535) Elemental Analysis: C=53.34(53.63);H=6.46(6.75);N=7.77(7.82) EXAMPLE 153: 3-(4-Aminobutyl)-1-[(3-fluorophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 153 is obtained from intermediate 21 and 3-fluorobenzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.48 (m, 1 H), 7.24 (m, 3 H), 4.31 (AB, 2 H), 3.71 / 3.35 (2m, 2 H), 3.45 / 3.12 (2m , 2 hrs), 2.92 (m, 2 hrs), 2.24 / 1.77 (2m, 2 hrs), 1.93 / 1.46 (2m, 2 hrs), 1.58 (quint., 2 hrs), 1.22 / 1.1 (2m, 2 hrs ) NMR 19 F: (300 MHz, D20) δ ppm -112 NMR 31 P: (300 MHz, D20) δ ppm 22.9 ESI / FIA / HR and MS / MS: [M+H]+ = 359.1536 (359.1535) Elemental Analysis: C=53.15(53.63);H=6.41(6.75);N=7.83(7.82) EXAMPLE 154: 3-(4-Aminobutyl)-1-[(6-aminopyridin-3-yl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 154 is obtained from intermediate 21 and 2-(Boc-amino)pyridine-5-carboxaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.97 (d, 1 H), 7.61 (dd, 1 H), 6.71 (d, 1 H), 4.18 (AB, 2 H), 3.67 / 3.29 (2m, 2 H), 3.42 / 3.05 (2m, 2H), 2.93 (m, 2H), 2.22 / 1.77 (2m, 2H), 1.93 / 1.47 (2m, 2H), 1.59 (quint., 2H), 1.25 / 1.11 (2m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 23.2 ESI / FIA / HR and MS / MS: [M+H]+ = 357.1696 (357.1691) Elemental Analysis: C=51.09(50.56);H=6.51(7.07);N=15.78(15.72) EXAMPLE 155: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-phenoxyphenyl)-methyl]-1,4-azaphosphinane-3-carboxylic acid Example 155 is obtained from intermediate 21 and 2-phenoxybenzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.47 (t, 1 H), 7.41 (t, 2 H), 7.27-7.09 (m, 4 H), 7.05 (d, 2 H), 4.27 (AB, 2 H), 3.68 / 3.3 (2m, 2H), 3.46 / 3.07 (2m, 2H), 2.91 (m, 2H), 2.23 / 1.76 (2m, 2H), 1.93 / 1.46 (2m, 2H) , 1.6 (quint., 2H), 1.15 (m, 2H) NMR 31 P: (300 MHz, D20) δ ppm 25.8 ESI / FIA / HR and MS / MS: [M+H]+ = 433.1894 (433.1892) Elemental Analysis: C=61.51(61.10);H=6.57(6.76);N=6.61(6.48) EXAMPLE 156: 3-(4-Aminobutyl)-1-[[2-(4-chlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 156 is obtained from intermediate 21 and 2-(4-chlorophenyl)benzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm Ί .611.5211 A (m, 3 H), 7.52 / 7.34 (2d, 4 H), 4.35 (AB, 2 H), 3.4 / 3.1 (2m, 2 H), 3.17 / 2.86 (2m, 2H), 2.94 (m, 2H), 2.09 / 1.64 (2m, 2H), 1.85 / 1.35 (2m, 2H), 1.58 (m, 2H), 1.08 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 451.1559 (451.1553) Elemental Analysis: C=58.24(58.60);H=5.82(6.26);N=6.48(6.21) EXAMPLE 157: 3-(4-Aminobutyl)-1-[(2-bromophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 157 is obtained from intermediate 21 and 2-bromobenzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.75 (dl, 1H), 7.53 (dd, 1H), 7.45 (tl, 1H), 7.39 (td, 1H), 4.44 (AB, 2H) , 3.74 / 3.43 (2m, 2H), 3.5 / 3.28 (2m, 2H), 2.94 (m, 2H), 2.24 / 1.79 (2m, 2H), 1.95 / 1.5 (2m, 2H), 1.6 (m, 2H), 1.26 / 1.1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 419.0732 (419.0735) Elemental Analysis: C=45.33(45.84);H=5.29(5.77);N=7.00(6.68) EXAMPLE 159: Acid 3-(4-aminobutyl)-4-hydroxy-4-oxo-1-[(2-oxo -l,3-dihydroindol- 5-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 159 is obtained from intermediate 21 and oxindole-5-carboxaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.35 (d, 1 H), 7.3 (dd, 1 H), 7 (d, 1 H), 4.35 / 4.15 (dd, 2 H), 3.7 / 3.3 (2m , 2H), 3.6 (dd, 2H), 3.4 / 3.1 (2dd, 2H), 2.9 (m, 2H), 2.2 / 1.75 (2m, 2H), 1.9 / 1.45 (2m, 2H) , 1.58 (m, 2H), 1.3-1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 396.1692 (396.1688) Elemental Analysis: C=54.70(54.68);H=6.42(6.63);N=10.57(10.63) EXAMPLE 160: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl]methyl]-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 160 is obtained from intermediate 21 and 2-(3-methyl-1,2,4-oxadiazol-5-yl)benzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.26 (d, 1H), 7.72 (m, 2H), 7.65 (d, 1H), 4.78 / 4.36 (2*d, 2H), 4 / 3.55 (m, 2H), 3.44 / 3.25 (m, 2H), 2.91 (m, 2H), 2.5 (s, 3H), 2.31 / 1.88 (m, 2H), 1.88 / 1.49 (m, 2 H), 1.58 (m, 2H), 1.22 / 1.02 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 423.1801 (423.1797) Elemental Analysis: C=53.57(54.02);H=6.25(6.44);N=12.77(13.26) EXAMPLE 161: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-[2-methyl-5- (trifluoromethyl)pyrazol-3-yl]phenyl]methyl]-4-oxo-1,4-azaphosphinan-3-carboxylic Example 156 is obtained from intermediate 21 and 2-[1-methyl-3(trifluoromethyl)-1H-pyrazol-5-yl]benzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.71 (d, 1H), 7.67 (t, 1H), 7.63 (t, 1H), 7.48 (d, 1H), 6.83 (s, 1H) , 4.3 / 4.18 (dl, 2H), 3.53 / 3.21 (m, 2H), 3.27 (s, 3H), 3.27 / 3.03 (m, 2H), 2.94 (m, 2H), 2.18 / 1.71 (m, 2H), 2.18 / 1.43 (m, 2H), 1.6 (m, 2H), 1.18 / 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 489.1903 (489.1878) Elemental Analysis: C=51.66(51.64);H=5.61(5.78);N=11.25(11.47) EXAMPLE 162: 3-(4-Aminobutyl)-1-[[2-(2,4-difluorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 162 is obtained from intermediates 21 and 287 according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.65 (m, 1 H), 7.57 (m, 2 H), 7.4 (m, 1 H), 7.34 (m, 1 H), 7.1 (2*m, 2 H), 4.45-4 (m, 2H), 3.7-2.8 (m, 2H), 3.7-2.8 (m, 2H), 2.93 (m, 2H), 2.15 / 1.66 (2*m, 2 H), 1.88 / 1.6 (2*m, 2H), 1.6 / 1.38 (2*m, 2H), 1.15 / 1.05 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 453.1745 (453.1754) Elemental Analysis: C=58.27(58.40);H=6.09(6.01);N=6.17(6.19) EXAMPLE 163: 3-(4-aminobutyl)-1-[[2-fluoro-6-(4-hydroxyphenyl) acid phenyl]-methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic Example 163 is obtained from intermediate 21 and 2-fluoro-6-(4-hydroxyphenyl)benzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.52 (m, 1H), 7.27 (m, 1H), 7.22 (d, 2H), 7.19 (m, 1H), 6.98 (d, 2H) , 4.41 (dd, 2 hrs), 3.45 / 3.09 (m, 2 hrs), 3.16 / 2.9 (m, 2 hrs), 2.94 (m, 2 hrs), 2.09 / 1.64 (m, 2 hrs), 1.86 / 1.35 (m, 2 hrs), 1.59 (m, 2 hrs), 1.08 (m, 2 hrs) ESI / FIA / HR and MS / MS: [M+H]+ = 451.1813 (451.1798) Elemental Analysis: C=58.33(58.66);H=5.35(6.27);N=6.49(6.22) EXAMPLE 164: 3-(4-Aminobutyl)-1-[[2-(1,3-benzodioxol-5-yl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan-3-acid carboxylic Example 164 is obtained from intermediates 21 and 279 according to procedures F and D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.2-7.9 (s, 3H), 7.45 (d, 1H), 7.3 (m, 2H), 7.15 (d, 1H), 6.95 (dd , 1H), 6.95 (s, 1H), 6.8 (dd, 1H), 6.05 (s, 2H), 3.5 (d, 1H), 3.4 (d, 1H), 2.9 (m, 1 H), 2.7 (t, 2H), 2.55 (m, 1H), 2.35 (m, 1H), 2.25 (m, 1H), 1.7 (m, 1H), 1.6-1 (m, 7 H) ESI / FIA / HR and MS / MS: [M+H]+ = 461.1854 (461.1841) Elemental Analysis: C=60.04(59.99);H=6.06(6.35);N=5.62(6.08) EXAMPLE 165: Acid 3-(4-aminobutyl)-4-hydroxy-1-[[2-(6-methoxypyridin- 3-yl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 165 is obtained from intermediate 21 and 2-(6-methoxy-3-pyridinyl)benzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 8.05 (s, 1H), 7.75 (dd, 1H), 7.6 (m, 1H), 7.5 (m, 2H), 7.35 (m, 1H) , 6.95 (d, 1H), 4.4 (d, 1H), 4.25 (d, 1H), 3.9 (s, 3H), 3.55-3.3 (m, 1H), 3.3-3.1 (m, 1 H), 3.1 (m, 1H), 2.95 (t, 2H), 2.85 (m, 1H), 2.1 (m, 1H), 1.85 (m, 1H), 1.75-1.5 (m, 3 H), 1.35 (m, 1H), 1.2-0.95 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 448.1996 (448.2001) Elemental Analysis: C=59.45(59.05);H=6.75(6.76);N=9.12(9.39) EXAMPLE 166: Acid 3-(4-aminobutyl)-4-hydroxy-4-oxo-1-[[2-( 6-Oxo-1H-pyridin-3-yl)phenyl]methyl]-1,4-azaphosphinane-3-carboxylic Example 166 is obtained from intermediates 21 and 237 according to procedures F and D previously described. 1H NMR: (300 / 400 MHz, D20) δ ppm 7.7 (dd, 1H), 7.6 (s, 1H), 7.6-7.3 (2*m, 2H), 6.7 (d, 1H), 4.35 (m, 2H), 3.6-3.4 (m, 1H), 3.4-3.05 (m, 2H), 3 (m, 1H), 2.9 (t, 2H), 2.1 (m, 1H) , 1.85 (m, 1H), 1.7 (m, 1H), 1.6 (m, 2H), 1.4 (m, 1H), 1.25-0.95 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 434.1860 (434.1844) Elemental Analysis: C=58.86(58.19);H=6.27(6.51);N=9.89(9.69) EXAMPLE 167: 3-(4-Aminobutyl)-4-hydroxy-1-[(2-imidazo[1,2-a]pyridin-3-ylphenyl)methyl]-4-oxo-1,4-azaphosphinan-3 acid -carboxylic Example 167 is obtained from intermediates 21 and 227 according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.98 (d, 1H), 7.68 (s, 1H), 7.65 (d, 1H), 7.65 (m, 2H), 7.52 (m, 1H) , 7.45 (dd, 1H), 7.22 (m, 1H), 6.98 (t, 1H), 4.25 (m, 2H), 3.45 / 3.1 (2*m, 2H), 2.9 (m, 2 H), 2.85 (m, 2H), 2.12 / 1.55 ​​(2*m, 2H), 1.8 / 1.55 ​​(2*m, 2H), 1.55 / 0.95 (2*m, 2H), 1.28 / 0.95 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 457.2004 (457.20046) Elemental Analysis: C=59.82(60.52);H=5.48(6.40);N=11.98(12.27) EXAMPLE 168: 3-(4-Aminobutyl)-1-[(2-chlorophenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 168 is obtained from intermediate 21 and 2-chlorobenzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.58 / 7.53 (2*d, 2 H), 7.48 / 7.4 (2*m, 2 H), 4.44 (m, 2 H), 3.71 / 3.41 (2*m, 2H), 3.51 / 3.28 (2*m, 2H), 2.94 (m, 2H), 2.22 / 1.78 (2*m, 2H), 1.95 / 1.61 (2*m, 2H), 1.6 / 1.49 (2*m, 2H), 1.28 / 1.11 (2*m, 2H) NMR 31 P: (400 MHz, D20) δ ppm -25.5 ESI / FIA / HR and MS / MS: [M+H]+ = 375.1235 (375.1240) Elemental Analysis: C=51.58(51.27);H=6.22(6.45);N=7.65(7.47) EXAMPLE 169: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(1R)-1-phenylethyl]-1,4-azaphosphinane-3-carboxylic acid Example 169 is obtained from intermediate 21 and acetophenone according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.5 (m, 5 H), 4.67 (quad., 1 H), 3.72 / 3.53 (2*m, 1 H), 3.62 / 3.41 (2*m, 1 H ), 3.29 / 3.13 (2*m, 1H), 3.09-2.9 (m, 1H), 3.09-2.9 (m, 2H), 2.28 / 2.11 (2*m, 1H), 2-1.65 ( m, 1H), 2-1.65 (m, 2H), 1.7 (2*d, 3H), 1.7-1.05 (m, 2H), 1.7-1.05 (m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 26.4 / 26.2 ESI / FIA / HR and MS / MS: [M+H]+ = 355.1783 (355.1786) Elemental Analysis: C=58.22(57.62);H=7.85(7.68);N=8.04(7.90) EXAMPLE 170: 3-(4-aminobutyl)-4-hydroxy-4-oxo-1-[(2-phenylphenyl) acid )methyl]-l,4-azaphosphinane-3-carboxylic acid Example 170 is obtained from intermediate 21 and 2-phenylbenzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.65-7.3 (m, 6H), 4.33 (AB, 2H), 3.43-3 (m, 3H), 2.92 (dd, 1H), 2.82 (m, 2H), 2.06 / 1.57 (2m, 2H), 1.83 / 1.33 (2m, 2H), 1.57 (m, 2H), 1.08 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 417.1945 (417.1943) Elemental Analysis: C=63.68(63.45);H=6.84(7.02);N=6.85(6.73) EXAMPLE 171: 3-(4-Aminobutyl)-1-[[2-(furan-3-yl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 171 is obtained from intermediates 21 and 290 according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.68 (m, 1H), 7.65 (m, 1H), 7.58-7.44 (m, 4H), 6.63 (m, 1H), 4.49 / 4.4 (2 *d, 2H), 3.5 / 3.22 (2*m, 2H), 3.34 / 3.01 (2*m, 2H), 2.94 (m, 2H), 2.1 / 1.68 (2*m, 2H) , 1.69 / 1.6 (2*m, 2H), 1.59 / 1.41 (2*m, 2H), 1.18 / 1.08 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 407.1736 (407.1735) Elemental Analysis: C=59.20(59.11);H=7.12(6.70);N=7.00(6.89) EXAMPLE 172: 3-(4-Aminobutyl)-4-hydroxy-1-[[2-(3-hydroxyphenyl)phenyl]-methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 172 is obtained from intermediates 21 and 281 according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.52 (m, 2 H), 7.39 (m, 1 H), 7.39 (m, 1 H), 7.29 (d, 1 H), 6.95 (dd, 1 H) , 6.9 (dl, 1H), 6.85 (si, 1H), 4.44 / 4.29 (d, 2H), 3.38 / 3.13 (m, 2H), 3.2 / 2.85 (m, 2H), 3.13 / 1.36 (m, 2H), 2.94 (m, 2H), 2.1-1.65 (m, 2H), 1.59 (m, 2H), 1.13 / 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 433.1895 (433.1892) Elemental Analysis: C=61.64(61.10);H=6.51(6.76);N=6.73(6.48) EXAMPLE 173: 3-(4-Aminobutyl)-1-[[2-(4-chlorophenyl)-4-fluorophenyl]-methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 173 is obtained from intermediates 21 and 220 according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.59 (dd, 1H), 7.51 (d, 2H), 7.32 (d, 2H), 7.23 (td, 1H), 7.14 (dd, 1H) , 4.3 (AB, 2H), 3.37 / 3.06 (2m, 2H), 3.11 / 2.81 (2m, 2H), 2.92 (m, 2H), 2.06 / 1.62 (2m, 2H), 1.83 / 1.33 (2m, 2H), 1.56 (m, 2H), 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 469.1470 (469.1459) Elemental Analysis: C=56.07(56.35);H=5.39(5.80);N=6.03(5.97) EXAMPLE 174: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-propan-2-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 174 is obtained from intermediate 21 and 2-isopropylbenzaldehyde according to procedures F and D previously described. 1H NMR: (500 MHz, D20) δ ppm 7.49 (d, 1H), 7.45 (t, 1H), 7.38 (d, 1H), 7.28 (t, 1H), 4.39 (dd, 2H) , 3.65 (dd, 1H), 3.5 (dd, 1H), 3.35 (m, 1H), 3.21 (dd, 1H), 3.09 (m, 1H), 2.91 (m, 2H), 2.17 (m, 1H), 1.93 (m, 1H), 1.74 (m, 1H), 1.58 (m, 2H), 1.47 (m, 1H), 1.24 (m, 1H), 1.2 / 1.18 (2*s, 6H), 1.1 (m, 1H) ESI / FIA / HR and MS / MS: [M+H]+ = 383.2097 (383.2099) Elemental Analysis: C=59.45(59.67);H=8.00(8.17);N=7.60(7.33) EXAMPLE 175: 3-(4-Aminobutyl)-1-[[2-(3,4-dichlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 175 is obtained from intermediates 21 and 215 according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.62 (d, 1H), 7.6 (m, 1H), 7.54 (d, 1H), 7.52 (m, 2H), 7.37 (m, 1H) , 7.24 (dd, 1H), 4.34 (AB, 2H), 3.45 / 3.07 (2m, 2H), 3.12 / 2.83 (2m, 2H), 2.93 (m, 2H), 2.1 / 1.63 (2m , 2H), 1.84 / 1.33 (2m, 2H), 1.57 (m, 2H), 1.04 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 485.1158 (485.1163) Elemental Analysis: C=54.91(54.44);H=5.37(5.61);N=5.35(5.77) EXAMPLE 176: 3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(3-phenylthiophen-2-yl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 176 is obtained from intermediates 21 and 284 according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.62 (d, 1H), 7.49 (t, 2H), 7.44 (t, 1H), 7.4 (d, 2H), 7.17 (d, 1H) , 4.6 (AB, 2H), 3.52 / 3.13 (2m, 2H), 3.13 / 2.73 (2m, 2H), 2.91 (m, 2H), 2.12 / 1.66 (2m, 2H), 1.81 / 1.26 (2m, 2H), 1.55 (m, 2H), 0.97 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 423.1525 (423.1507) Elemental Analysis: C=56.76(56.86);H=6.46(6.44);N=7.19(6.63);S=7.30(7.59) Procedure G: Chiral Separation of Intermediate 20b Diastereoisomers Intermediate 128: tert-Butyl (3S)-3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-1-benzyl-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate DMSO (30 mL) and 60% NaH (6.78 g, 186.6 mmol, 1.6 eq) are successively introduced under an argon atmosphere into a three-necked IL flask equipped with mechanical stirring. The flask is maintained at room temperature using a water bath. A solution of intermediate 204 (41.1 g, 116.7 mmol, 1.1 eq) in DMSO (25 mL) is then added dropwise over 5 minutes. A solution of intermediate 19 (37.54 g, 106 mmol) in DMSO (100 mL) is then added dropwise while maintaining the temperature below 20°C. Indeed, the addition causes a significant heating as well as a strong thickening of the reaction medium. After the end of the addition, 100 mL of anhydrous THF are then added in order to be able to maintain stirring. After 3 h, the reaction mixture is cooled using an ice water bath and hydrolyzed by adding 500 mL of a solution saturated with NH 4 C1. The mixture is then extracted with AcOEt (3 x 300 mL). The organic phases are then combined, washed with a saturated NaCl solution (2 x 300 mL), and dried over MgSC 4 before being concentrated under reduced pressure to yield a yellowish solid (69.94 g), a mixture of 4 diastereoisomers. The 4 diastereoisomers of intermediate 20b are separated on a chiral column of type (i?,i?)-Whelk-0-1 of 2.5 kg per batch of 8 g, each batch requiring 2 passages under the following conditions: 1 er passage : The mixture containing the 4 diastereoisomers of intermediate 20b (8 g of crude) is deposited on a chiral column of type (i?,i?)-Whelk-0-1 of 2.5 kg using DCM / Heptane as mobile phase ( 55:45) + 10% NAnd 3 in order to isolate the diastereoisomer 4 (number assigned according to the order of leaving the column) of the intermediate 20b. The mixture containing the 3 remaining diastereoisomers of intermediate 20b is loaded onto a 2.5 kg (i?,i?)-Whelk-0-1 chiral column using MTBE + 10% DEA as mobile phase in order to isolate the diastereoisomer 2. After 9 injections, the fractions containing diastereoisomers 2 and 4 of intermediate 20b are then combined and evaporated under reduced pressure to yield intermediate 128 (25.2 g, 40.3 mmol), quaternary carbon of configuration (S) with a yield by 38%. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.3 (m, 5 H), 4 (m, 2 H), 3.6 (d, 1 H), 3.4 (d, 1 H), 3.35 (m, 2 H), 2.9 (m, 1H), 2.8 (dd, 1H), 2.45 (dd, 1H), 2.3 (m, 1H), 1.9 (m, 4H), 1.4 (m, 2H), 1.38 (s, 18H), 1.35 (s, 9H), 1.2 (t, 3H), 0.8 (3, 2H). IRcm "1 ): 1760-1680cm "1 (C=0), 1124cm "1 (P=0), 1124 cm^C-O-C). Intermediate 129: tert-Butyl (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate In a flask of 500 mL at room temperature and under argon flow are successively introduced intermediate 128 (30.35 g, 48.6 mol), ethanol (200 mL), Pd / C (3.03 g, 10%) by weight) and 37% HCl > (3 mL, 0.8eq). The argon is then replaced by an atmosphere of hydrogen. The reaction is monitored by LC / MS. After 4 hours, the reaction is complete and the catalyst is filtered through fiberglass The filtrate is evaporated to dryness to obtain a yellow oil which is taken up in AcOEt (200 mL) and in a solution of NaHC0 3 at 10% > (200 mL). After decantation, the aqueous phase is extracted with AcOEt (3×100 mL). The organic phases are combined then washed with a saturated NaCl solution (400 mL), dried over MgS0 4 and concentrated to yield intermediate 129 in the form of a white solid (23.12 g, 43.24 mmol) with a yield of 89%. 1H NMR: (DMSO-dg, 400 MHz) δ 4.01 to 3.88 (m, 2H), 3.47 (m, 2H), 2.95-2.68 (2m, 2H), 2.95 (m, 2H), 2.23 ( m, 1H), 1.92-1.68 (m, 4H), 1.48 (m, 2H), 1.44 (s, 9H), 1.41 (s, 9H), 1.3 (s, 9H), 1.27 / 0.97 (2m, 2H), 1.24 / 0.97 (2t, 3H). IR Ccm 1 ): 1715-1692cm "1 (C=0), 1125 cm^C-O-C). EXAMPLE 177: (3S)-3-(4-Aminobutyl)-1-benzyl-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 177 is obtained from intermediate 128 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.49 (m, 5H), 4.41 / 4.21 (2d, 2H), 3.7 / 3.32 (2m, 2H), 3.5 / 3.1 (2m, 2H), 2.91 (m, 2H), 2.22 / 1.78 (2m, 2H), 1.92 (m, 1H), 1.6 (m, 2H), 1.45 (m, 1H), 1.22 / 1.1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 341.1638 (341.1630) Elemental Analysis: C=56.43(56.46);H=7.33(7.40);N=8.20(8.23) PR: -45.630 (589 nm, T=20°C, C=1.1) Intermediate 131: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-1-[[2-(3,4-dimethoxyphenyl)-4-fluorophenyl]methyl]-4-ethoxy tert-Butyl -4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 131 is obtained from intermediates 129 and 229 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.5 (dd, 1H), 7.15 (m, 1H), 7.05 (m, 2H), 6.9 (m, 2H), 3.95 (m, 2 H), 3.8 (2s, 6H), 3.55 (d, 1H), 3.35 (d, 1H), 3.3 (m, 2H), 2.85-2.65 (m, 2H), 2.35 (dd, 1 H), 2.25 (m, 1H), 2-1.75 (m, 4H), 1.45-1.3 (m, 2H), 1.4 (s, 18H), 1.35 (s, 9H), 1.2 (t , 3H), 0.8-0.6 (m, 2H). EXAMPLE 179: (3S)-3-(4-Aminobutyl)-1-[[2-(3,4-dimethoxyphenyl)-4-fluorophenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane acid -3- carboxylic Example 179 is obtained from intermediate 131 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.6 (dd, 1H), 7.2 (td, 1H), 7.1 (m, 1H), 7 (dd, 1H), 6.9 (dd, 1H) , 4.4 / 4.25 (2d, 2H), 3.8 (2s, 6H), 3.35 (m, 1H), 3.2-2.75 (m, 5H), 2.05 (m, 1H), 1.8 (m , 1H), 1.6 (m, 3H), 1.3 (m, 1H), 1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 495.2056 (495.2060) Elemental Analysis: C=58.64(58.29);H=6.44(6.52);N=5.72(5.67) PR: -23.170 (589nm, T=21°C, C=0.8) Intermediate 132: (3S)-3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-fluoro-2-(4-methylphenyl)phenyl]methyl]- 4-oxo-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 132 is obtained from intermediates 129 and 272 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.51 (dd, 1H), 7.26 (s, 4H), 7.18 (td, 1H), 7.01 (dd, 1H), 3.93 (m, 2 H), 3.42 (AB, 2H), 3.34 (m, 2H), 2.72 / 2.2 (2m, 2H), 2.72 / 2.32 (2m, 2H), 2.36 (s, 3H), 1.9-1.7 (m, 4H), 1.41 (s, 18H), 1.37 (m, 2H), 1.34 (s, 9H), 1.17 (t, 3H), 0.7 (m, 2H) EXAMPLE 180: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(4-methylphenyl)phenyl]-methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane acid -3-carboxylic Example 180 is obtained from intermediate 132 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.61 (dd, 1H), 7.36 (d, 2H), 7.26 (d, 2H), 7.23 (td, 1H), 7.15 (dd, 1H) , 4.41 / 4.26 (2*d, 2H), 3.35 / 3.09 (m, 2H), 3.17 / 2.81 (m, 2H), 2.95 (m, 2H), 2.37 (s, 3H), 2.08 / 1.64 (m, 2H), 1.85 / 1.35 (m, 2H), 1.6 (m, 2H), 1.13 / 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 449.2005 (449.2005) Elemental Analysis: C=61.57(61.60);H=6.53(6.74);N=6.45(6.25) PR: -15.640 (589nm, T=20°C, C=1.0) Intermediate 133: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-phenylphenyl)methyl]-1,4-azaphosphinane tert-Butyl -3-carboxylate Intermediate 133 is obtained from intermediate 129 and 2-phenylbenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.52-7.2 (m, 9H), 4.06-3.86 (m, 2H), 3.55 / 3.36 (AB, 2H), 3.36 (m, 2H) , 2.71 / 2.32 / 2.19 (3m, 4H), 1.95-1.65 (m, 4H), 1.42 / 1.34 (2s, 27H), 1.37 (m, 2H), 1.21 / 1.17 (2t, 3H) , 0.68 (m, 2H) EXAMPLE 181: (3S)-3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-phenylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 181 is obtained from intermediate 133 according to procedure D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.65-7.3 (m, 9H), 4.3 (AB, 2H), 3.43 / 3 (m, 3H), 2.92 (dd, 1H), 2.82 (m, 2 hrs), 2.06-1.57 (2m, 2 hrs), 1.83 / 1.33 (2m, 2 hrs) 1.57 (m, 2 hrs), 1.08 (m, 2 hrs) ESI / FIA / HR and MS / MS: [M+H]+ = 417.1938 (417.1943) Elemental Analysis: C=62.99(63.45);H=6.45(7.02);N=6.93(6.73) Intermediate 134: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-pyrimidin-5-ylphenyl)methyl]-1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 134 is obtained from intermediates 129 and 236 according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 9.2 (s, 1H), 8.85 (s, 2H), 7.45 (m, 3H), 7.35 (d, 1H), 3.95 (m, 2 H), 3.55 (d, 1H), 3.4 (d, 1H), 3.3 (m, 2H), 2.8-2.55 (m, 2H), 2.45-2.15 (2*m, 2H), 2.15 -1.7 (m, 2H), 2-1.55 (m, 4H), 1.5-1.25 (3s, 27H), 1.2 (t, 3H), 0.6 (m, 2H) EXAMPLE 182: (3S)-3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-pyrimidin-5-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 182 is obtained from intermediate 134 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 9.15 (s, 1H), 8.82 (s, 2H), 7.7-7.55 (m, 3H), 7.43 (d, 1H), 4.4 / 4.3 (2d , 2H), 3.6-3.35 (m, 1H), 3.3-3.1 (m, 1H), 3.1 (m, 1H), 2.95 (m, 3H), 2.1 (m, 1H), 1.85 (m, 1H), 1.65 (m, 1H), 1.62-1.45 (m, 2H), 1.35 (m, 1H), 1.15-1 (m, 2H) ESI / FIA HR and MS / MS: [M+H]+ = 419.1855 (419.1848) Elemental Analysis: C=57.01(57.41);H=6.57(6.50);N=13.45(13.39) PR: -20.520 (589nm, T=20°C, C=1.0) Intermediate 135: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-thiophen-2-ylphenyl)methyl]-1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 135 is obtained from intermediate 129 and 2-(2-thienyl)benzaldehyde according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.62 (d, 1H), 7.45-4.3 (m, 4H), 7.25 (d, 1H), 7.15 (t, 1H), 4.1-3.9 (quad., 2 hrs), 3.65 / 3.45 (d, 2 hrs), 3.4-3.2 (m, 2 hrs), 2.9-2.7 (m, 2 hrs), 2.4-2.3 (m, 2 hrs), 1.9- 1.7 (m, 4H), 1.5-1.3 (m, 2H), 1.4 / 1.35 (2*s, 27H), 1.2 (t, 3H), 0.7-0.5 (m, 2H) EXAMPLE 183: (3S)-3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-thiophen-2-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid Example 183 is obtained from intermediate 135 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.6 (d, 1H), 7.55 (d, 1H), 7.48 (m, 2H), 7.45 (d, 1H), 7.15 (dd, 1H) , 7.1 (t, 1H), 4.5 / 1.4 (2*d, 2H), 3.5-3.2 (m, 3H), 3-2.85 (m, 3H), 2.15 / 1.7 (m, 4H) , 1.88 (m, 1H), 1.55 (m, 2H), 1.2-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 423.1505 (423.1507) Elemental Analysis: C=57.14(56.86);H=6.12(6.44);N=6.61(6.63);S=7.33(7.59) PR: -18.340 (589nm, T=20°C, C=0.9) Intermediate 136: (3S)-3-{4-[Bis(tef"f-butoxtcarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-[(2-pyridin-3-ylphenyl)methyl]-1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 136 is obtained from intermediates 129 and 260 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.59 (dd, 1H), 8.56 (dd, 1H), 7.82 (dt, 1H), 7.49 (dd, 1H), 7.48 (dd, 1 H), 7.42 / 7.39 (2td, 2H), 7.27 (dd, 1H), 3.92 (m, 2H), 3.44 (AB, 2H), 3.3 (m, 2H), 2.7 / 2.2 (2m , 2H), 2.7 / 2.35 (2m, 2H), 1.95-1.66 (m, 4H), 1.42 (s, 18H), 1.35 (m, 2H), 1.33 (s, 9H), 1.17 (t, 3H), 0.63 (m, 2H) EXAMPLE 184: (3S)-3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-pyridin-3-ylphenyl)methyl]-1,4-azaphosphinane-3-carboxylic acid example 184 is obtained from intermediate 136 according to procedure D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.57 (d, 1H), 8.48 (s, 1H), 7.83 (d, 1H), 7.65 (m, 1H), 7.57 (m, 1 H), 7.57 (m, 2H), 7.4 (m, 1H), 4.41 / 4.29 (dd, 2H), 3.44 / 3.12 (dd, 2H), 3.2 / 2.86 (dd, 2H), 2.93 (m, 2H), 2.1 / 1.67 (2*m, 2H), 1.85 / 1.35 (2*m, 2H), 1.59 (m, 2H), 1.08 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 418.1871 (418.1895) Elemental Analysis: C=60.35(60.42);H=6.74(6.76);N=9.70(10.07) PR: -20.940 (589nm, T=28°C, C=0.9) Intermediate 137: (3S)-3-{4-[Bis(tert-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-fluoro-2-(3-methoxyphenyl)phenyl]methyl]-4- tert-Butyl oxo-1,4-azaphosphinane-3-carboxylate Intermediate 137 is obtained from intermediates 129 and 222 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.51 (dd, 1H), 7.36 (t, 1H), 7.2 (td, 1H), 7.05 (dd, 1H), 6.97 (d, 1 H), 6.91 (m, 1H), 6.9 (m, 1H), 3.93 (m, 2H), 3.79 (s, 3H), 3.52 / 3.33 (2*d, 2H), 3.33 (m , 2H), 2.72 / 2.21 (m, 2H), 2.72 / 2.32 (m, 2H), 2-1.75 (m, 4H), 1.4 (s, 18H), 1.37 (m, 2H) , 1.34 (s, 9H), 1.17 (t, 3H), 0.69 (m, 2H) EXAMPLE 185: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(3-methoxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane- 3-carboxylic Example 185 is obtained from intermediate 137 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.62 (dd, 1H), 7.46 (t, 1H), 7.25 (td, 1H), 7.16 (dd, 1H), 7.08 (dd, 1H) , 6.97 (dl, 1H), 6.96 (si, 1H), 4.41 / 4.27 (2*d, 2H), 3.84 (s, 3H), 3.37 / 3.09 (m, 2H), 3.16 / 2.83 (m, 2H), 2.95 (m, 2H), 2.09 / 1.66 (m, 2H), 1.86 / 1.35 (m, 2H), 1.66 (m, 2H), 1.13 / 1.06 (m, 2 h) ESI / FIA / HR and MS / MS: [M+H]+ = 465.1941 (465.1949) Elemental Analysis: C=59.94(59.48);H=6.44(6.51);N=6.11(6.03) PR: -19.240 (589nm, T=20°C, C=0.6) Intermediate 138: (3S)-3-{4-[Bis(tef"f-butoxycarbonyl)amino]butyl}-1-[[3-(4-chlorophenyl)pyridin-2-yl]methyl]-4-ethoxy- tert-Butyl 4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 138 is obtained from intermediates 129 and 291 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.55 (d, 1H), 7.68 (d, 1H), 7.55 (m, 4H), 7.42 (dd, 1H), 3.94 (m, 2 H), 3.63 / 3.44 (2*d, 2H), 3.19 (m, 2H), 2.98 / 2.51 (2*m, 2H), 2.64 / 2.36 (2*m, 2H), 1.91 / 1.75 (2*m, 2H), 1.75 / 1.62 (2*m, 2H), 1.4 (s, 18H), 1.33 (s, 9H), 1.23 (m, 2H), 1.18 (t, 3 H), 0.59 / 0.34 (m, 2H) EXAMPLE 186: (3S)-3-(4-Aminobutyl)-1-[[3-(4-chlorophenyl)pyridin-2-yl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan- 3-carboxylic Example 186 is obtained from intermediate 138 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.6 (d, 1H), 7.8 (d, 1H), 7.5 (m, 3H), 7.3 (d, 2H), 4.4 (m, 2H) , 3.5-3.3 (m, 2H), 3.2 (m, 2H), 2.95 (m, 2H), 2.2 (m, 1H), 1.9 (m, 1H), 1.65 (m, 1H) , 1.6 (m, 2H), 1.45 (m, 1H), 1.3-1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 452.1502 (452.1500) Elementary Analysis: C=55.89(55.82);H=5.56(6.02);N=9.17(9.30) PR: -5.260 (589nm, T=20°C, C=1.0) Intermediate 139: (3S)-3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-fluoro-2-(4-methoxyphenyl)phenyl]methyl]-4- tert-Butyl oxo-1,4-azaphosphinane-3-carboxylate Intermediate 139 is obtained from intermediates 129 and 221 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.49 (dd, 1H), 7.31 (d, 2H), 7.17 (m, 1H), 7.01 (m, 1H), 7.01 (d, 2 H), 3.93 (m, 2H), 3.8 (s, 3H), 3.5 / 3.32 (2*d, 2H), 3.32 (m, 2H), 2.75 / 2.21 (2*m, 2H) , 2.72 / 2.33 (2*m, 2H), 2-1.78 (massive, 2H), 2-1.78 (massive, 2H), 1.4 / 1.33 (2*s, 27H), 1.38 (m, 2 H), 1.18 (t, 3H), 0.7 (m, 2H) EXAMPLE 187: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(4-methoxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane- 3-carboxylic Example 187 is obtained from intermediate 139 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.57 (dd, 1H), 7.3 (d, 2H), 7.19 (td, 1H), 7.12 (dd, 1H), 7.08 (d, 2H) , 4.32 (AB, 2H), 3.84 (s, 3H), 3.33 / 3.07 (2m, 2H), 3.13 / 2.8 (2m, 2H), 2.92 (m, 2H), 2.05 / 1.62 (2m , 2H), 1.83 / 1.32 (2m, 2H), 1.57 (m, 2H), 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 465.1960 (465.1954) Elemental Analysis: C=59.41(59.48);H=6.76(6.51);N=6.09(6.03) PR: -13.770 (589nm, T=20°C, C=0.9) Intermediate 140: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(4-methylphenyl)phenyl]methyl]-4-oxo- tert-butyl l,4-azaphosphinane-3-carboxylate Intermediate 140 is obtained from intermediates 129 and 288 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.49 (dd, 1H), 7.33 (2*m, 2H), 7.23 (2*d, 4H), 7.18 (dd, 1H), 3.92 (m, 2H), 3.54 / 3.35 (2*d, 2H), 3.3 (m, 2H), 2.74 / 2.2 (2*m, 2H), 2.74 / 2.32 (2*m, 2H) , 2.36 (s, 3H), 1.95-1.75 (m, 2H), 1.95-1.75 (m, 2H), 1.41 / 1.33 (2*s, 27H), 1.38 (m, 2H), 1.17 (t, 3 H), 0.71 (m, 2 H) EXAMPLE 188: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[[2-(4-methylphenyl)phenyl]methyl] acid - 4-oxo-1,4-azaphosphinane-3-carboxylic Example 188 is obtained from intermediate 140 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.6-7.35 (m, 4H), 7.33 / 7.22 (2d, 4H), 4.33 (AB, 2H), 3.33 / 3.07 (2m, 2H), 3.19 / 2.8 (2m, 2H), 2.91 (m, 2H), 2.35 (s, 3H), 2.06 / 1.58 (2m, 2H), 1.82 / 1.32 (2m, 2H), 1.57 (m, 2H), 1.07 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 431.2097 (431.2099) Elemental Analysis: C=64.03(64.17);H=6.92(7.26);N=6.45(6.51) PR_: -13.150 (589 nm, T=20°C, C=0.9) Intermediate 141: (3S)-3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-fluoro-2-(4-fluorophenyl)phenyl]methyl]-4- tert-Butyl oxo-1,4-azaphosphinane-3-carboxylate Intermediate 141 is obtained from intermediates 129 and 271 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.49 (dd, 1H), 7.42 (dd, 2H), 7.29 (t, 2H), 7.21 (td, 1H), 7.06 (dd, 1 H), 3.92 (m, 2H), 3.49 / 3.32 (2*d, 2H), 3.32 (m, 2H), 2.71 / 2.2 (2*m, 2H), 2.7 / 2.34 (2*m , 2 hrs), 1.9-1.65 (m, 2 hrs), 1.9-1.65 (m, 2 hrs), 1.4 / 1.33 (2*s, 27 hrs), 1.38 (m, 2 hrs), 1.18 (t, 3 H), 0.67 (m, 2 H) EXAMPLE 189: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(4-fluorophenyl)phenyl]-methyl]-4-hydroxy acid -4-oxo-1,4-azaphosphinane-3-carboxylic Example 189 is obtained from intermediate 141 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.59 (dd, 1H), 7.35 (m, 2H), 7.23 (td, 1H), 7.23 (t, 2H), 7.14 (dd, 1H) , 4.31 (AB, 2H), 3.36 / 3.07 (2m, 2H), 3.16 / 2.83 (2m, 2H), 2.92 (m, 2H), 2.06 / 1.58 (2m, 2H), 1.84 / 1.33 (2m, 2h), 1.58 (m, 2h), 1.07 (m, 2h) NMR 19 F: (300 MHz, D20) δ ppm -1 1 1.4 / -1 14.1 ESI / FIA / HR and MS / MS: [M+H]+ = 453.1750 (453.1754^ Elemental Analysis: C=58.26(58.40);H=5.79(6.01);N=6.18(6.19) PR: -17.770 (589nm, T=20°C, C=1.2) Intermediate 142: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-fluoro-2-pyridin-3-ylphenyl)methyl]-4 tert-Butyl -oxo-1,4-azaphosphinane-3-carboxylate Intermediate 142 is obtained from intermediates 129 and 261 according to procedure F previously described. NMR Ή: (400 MHz, dmso-d6) δ ppm 8.6 (dd, 1H), 8.58 (dl, 1H), 7.84 (dt, 1H), 7.51 (m, 2H), 7.26 (td, 1 H), 7.15 (dd, 1H), 3.93 (m, 2H), 3.42 (AB, 2H), 3.33 (m, 2H), 2.67 / 2.2 (2m, 2H), 2.67 / 2.35 (2m , 2H), 1.96-1.62 (m, 4H), 1.41 (s, 18H), 1.36 (m, 2H), 1.34 (s, 9H), 1.17 (t, 3H), 0.65 (m , 2H) EXAMPLE 190: (3S)-3-(4-Aminobutyl)-1-[(4-nuoro-2-pyridin-3-ylphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan-3-acid - carboxylic Example 190 is obtained from intermediate 142 according to procedure D previously described. NMR Ή: (300 MHz, D20) δ ppm 8.62 (dd, 1H), 8.54 (d, 1H), 7.89 (dt, 1H), 7.7 (dd, 1H), 7.6 (dd, 1H) , 7.34 (td, 1H), 7.23 (dd, 1H), 4.35 (AB, 2H), 3.46 / 3.12 (2m, 2H), 3.18 / 2.87 (2m, 2H), 2.97 (m, 2 H), 2.12 / 1.67 (2m, 2H), 1.88 / 1.37 (2m, 2H), 1.61 (m, 2H), 1.1 1 (m, 2H) NMR 19 F: (300 MHz, D20) δ ppm -111 ESI / FIA / HR and MS / MS: [M+H]+ = 436.1794 (436.1801) Elemental Analysis: C=57.69(57.93);H=5.69(6.25);N=9.60(9.65) PR: -19.680 (589 nm, T=20°C, C=0.7) Intermediate 143: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-methoxy-2-phenylphenyl)methyl]-4-oxo-1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 143 is obtained from intermediates 129 and 285 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.47-7.32 (m, 5H), 7.35 (d, 1H), 6.95 (dd, 1H), 6.75 (d, 1H), 3.92 (quad ., 2H), 3.77 (s, 3H), 3.47 / 3.27 (dd, 2H), 3.32 (t, 2H), 2.75 / 2.28 (dd, 2H), 2.67 / 2.16 (dd, 2H ), 1.85 / 1.72 (dd, 2H), 1.79 (t, 2H), 1.41 (s, 18H), 1.36 (m, 2H), 1.34 (s, 9H), 1.16 (t, 3H ), 0.68 (m, 2 H) EXAMPLE 191: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[(4-hydroxy-2-phenylphenyl)methyl]-4-oxo-1-acid, 4-azaphosphinane-3-carboxylic Example 191 is obtained from intermediate 143 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.54-7.44 (m, 3H), 7.54-7.44 (m, 1H), 7.34 (d, 2H), 6.97 (dd, 1H), 6.86 (df , 1H), 4.34 / 4.19 (2*d, 2H), 3.33 / 3.05 (2*m, 2H), 3.19 / 2.78 (2*m, 2H), 2.95 (m, 2H), 2.07 / 1.63 (2*m, 2H), 1.85 / 1.35 (2*m, 2H), 1.59 (m, 2H), 1.2-1 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 433.1887 (433.1887) Elemental Analysis: C=60.81(61.10);H=6.31(6.76);N=6.49(6.48) PR: -39.130 (589 nm, T=20°C, C=0.9) Intermediate 144: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1- tert-Butyl [(4-fluoro-2-pyridin-4-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 144 is obtained from intermediates 129 and 262 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.65 (m, 2 H), 7.53 (dd, 1 H), 7.44 (m, 2 H), 7.28 (td, 1 H), 7.14 (dd, 1 H), 3.93 (m, 2H), 3.44 (AB, 2H), 3.32 (m, 2H), 2.69 / 2.21 (2m, 2H), 2.69 / 2.35 (2m, 2H), 1.96-1.62 (m, 4H), 1.41 (s, 18H), 1.36 (m, 2H), 1.33 (s, 9H), 1.17 (t, 3H), 0.66 / 0.58 (2m, 2H) EXAMPLE 192: (3S)-3-(4-Aminobutyl)-1-[(4-fluoro-2-pyridin-4-ylphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan-3-acid - carboxylic Example 192 is obtained from intermediate 144 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.63 (d, 2H), 7.67 (dd, 1H), 7.45 (d, 2H), 7.33 (td, 1H), 7.21 (dd, 1H) , 4.4 / 4.29 (2*d, 2H), 3.44 / 3.08 (m, 2H), 3.16 / 2.88 (m, 2H), 2.95 (m, 2H), 2.1 / 1.65 (m, 2H) , 1.86 / 1.36 (m, 2H), 1.6 (m, 2H), 1.08 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 436.1804 (436.1801) Elemental Analysis: C=58.11(57.93);H=5.71(6.25);N=9.79(9.65) PR: -16.250 (589nm, T=20°C, C=1.0) Intermediate 146: (3S)-3-{4-[Bis(ter^butoxycarbonyl)amino]butyl}-1-[[2-(3-chlorophenyl)phenyl]methyl]-4-ethoxy-4-oxo-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 146 is obtained from intermediates 129 and 213 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.52 (si, 1H), 7.45 (m, 2H), 7.45 / 7.38 / 7.25 (3m, 4H), 7.33 (dt, 1H), 3.94 (m, 2H), 3.53 / 3.32 (AB, 2H), 3.25 (m, 2H), 2.76 / 2.37 (2m, 2H), 2.7 / 2.25 (2m, 2H), 1.95 / 1.78 (2m , 2H), 1.82 / 1.75 (2m, 2H), 1.41 (s, 18H), 1.33 (s, 9H), 1.33 (m, 2H), 1.18 (t, 3H), 0.66 / 0.57 (2m, 2H) EXAMPLE 194: (3S)-3-(4-Aminobutyl)-1-[[2-(3-chlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 194 is obtained from intermediate 146 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.63-7.23 (m, 8H), 4.33 (AB, 2H), 3.42 / 3.1 (2m, 2H), 3.17 / 2.82 (2m, 2H), 2.93 (m, 2H), 2.1 / 1.63 (2m, 2H), 1.84 / 1.34 (2m, 2H), 1.57 (m, 2H), 1.07 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 451.1539 (451.1548) Elemental Analysis: C=58.76(58.60);H=6.46(6.26);N=6.38(6.21) PR: -15.780 (589nm, T=20°C, C=1.2) Intermediate 147: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-1-[[4-chloro-2-(4-chlorophenyl)phenyl]methyl]-4-ethoxy- tert-Butyl 4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 147 is obtained from intermediates 129 and 292 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.52 (d, 2H), 7.5 (d, 1H), 7.45 (dd, 1H), 7.41 (d, 2H), 7.27 (d, 1 H), 3.94 (m, 2H), 3.5 / 3.33 (dd, 2H), 3.3 (m, 2H), 2.8-2.6 (2m, 2H), 2.35 (dd, 1H), 2.2 (m , 1H), 2-1.7 (m, 4H), 1.41 (s, 18H), 1.4-1.3 (m, 2H), 1.33 (s, 9H), 1.18 (t, 3H), 0.68 (m, 2H) EXAMPLE 195: (3S)-3-(4-Aminobutyl)-1-[[4-chloro-2-(4-chlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane- 3-carboxylic Example 195 is obtained from intermediate 147 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.55-7.5 (2d, 2H), 7.5 (d, 2H), 7.4 (d, 1H), 7.28 (d, 2H), 4.3 (dd, 2 H), 3.35 / 3.05 (2m, 2H), 3.15 / 2.8 (2m, 2H), 2.9 (m, 2H), 2.05 / 1.65 (2m, 2H), 1.8 / 1.3 (2m, 2H) , 1.55 (m, 2H), 1.05 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 485.1162 (485.1163) Elemental Analysis: C=55.11(54.44);H=5.26(5.61);N=5.87(5.77) PR: -17.410 (589nm, T=19°C, C=1.0) Intermediate 148: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[2-(6-methoxypyridin-3-yl)benzyl]-4-oxo tert-butyl 1,4-azaphosphinane-3-carboxylate Intermediate 148 is obtained from intermediates 129 and 237 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.1 (d, 1H), 7.75 (dd, 1H), 7.5-7.2 (m, 4H), 6.9 (d, 1H), 3.9 (s , 3H), 3.9 (m, 2H), 3.55 / 3.35 (dd, 2H), 3.3 (m, 2H), 2.75 / 2.2 (2m, 2H), 2.7 / 2.35 (2dd, 2H), 1.9 / 1.8 (2m, 2H), 1.8 (m, 2H), 1.4 (s, 18H), 1.35 (m, 2H), 1.35 (s, 9H), 1.2 (t, 3H), 0.65 (m, 2H) EXAMPLE 196: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[2-(6-methoxypyridin-3-yl)benzyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 196 is obtained from intermediate 148 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.05 (d, 1H), 7.75 (dd, 1H), 7.6 (m, 1H), 7.5 (m, 2H), 7.4 (m, 1H) , 7 (d, 1H), 4.3 (dd, 2H), 3.9 (s, 3H), 3.45 / 3.15 (2m, 2H), 3.2 / 2.85 (2dd, 2H), 2.9 (m, 2 H), 2.1 / 1.7 (2m, 2H), 1.8 / 1.35 (2m, 2H), 1.6 (m, 2H), 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 448.2009 (448.2001) Elemental Analysis: C=58.81(59.05);H=6.79(6.76);N=9.31(9.39) PR: -11.510 (589nm, T=19°C, C=0.9) Intermediate 149: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(4-fluorophenyl)phenyl]methyl]-4-oxo- tert-Butyl 1,4-azaphosphinane-3-carboxylate Intermediate 149 is obtained from intermediate 129 and 2-(4-fluorophenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.47 (dd, 1H), 7.39 / 7.33 (2*m, 2H), 7.39 (dd, 2H), 7.27 (t, 2H), 7.21 (dd, 1H), 3.93 (m, 2H), 3.52 / 3.34 (2*d, 2H), 3.38-3.22 (m, 2H), 2.75 / 2.21 (2*m, 2H), 2.7 / 2.35 (2*m, 2H), 1.98-1.72 (m, 2H), 1.98-1.72 (m, 2H), 1.41 / 1.34 (2*s, 27H), 1.37 (m, 2H) , 1.19 (t, 3H), 0.68 (m, 2H) EXAMPLE 197: (3S)-3-(4-Aminobutyl)-1-[[2-(4-fluorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 197 is obtained from intermediate 149 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.6 (d, 1H), 7.52 (m, 2H), 7.4 (d, 1H), 7.35 (dd, 2H), 7.24 (dd, 2H) , 4.41 / 4.29 (dd, 2H), 3.39 / 3.1 (2*m, 2H), 3.19 / 2.88 (2*m, 2H), 2.93 (m, 2H), 2.09 / 1.65 (2*m , 2H), 1.85 / 1.59 (2*m, 2H), 1.59 / 1.35 (2*m, 2H), 1.2-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 435.1843 (435.1843) Elemental Analysis: C=60.70(60.82);H=6.56(6.50);N=6.49(6.45) PR: -23.350 (589nm, T=20°C, C=0.7) Intermediate 150: (3S)-3-{4-[Bis(ter^butoxycarbonyl)amino]butyl}-1-[[2-(4-chlorophenyl)-4-fluorophenyl]methyl]-4-ethoxy-4-oxo - tert-Butyl 1,4-azaphosphinane-3-carboxylate Intermediate 150 is obtained from intermediates 129 and 220 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.52 (d, 2H), 7.5 (m, 1H), 7.42 (d, 2H), 7.22 (dt, 1H), 7.07 (dd, 1 H), 4-3.86 (m, 2H), 3.5 / 3.32 (2*d, 2H), 3.4-3.25 (m, 2H), 2.71 / 2.21 (2*m, 2H), 2.71 / 2.35 (2*m, 2H), 1.99-1.72 (m, 2H), 1.99-1.72 (m, 2H), 1.41 / 1.33 (2*s, 27H), 1.38 (m, 2H), 1.19 (t, 3H), 0.68 (m, 2H) EXAMPLE 198: (3S)-3-(4-Aminobutyl)-1-[[2-(4-chlorophenyl)-4-fluorophenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan-3 acid - carboxylic Example 198 is obtained from intermediate 150 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.62 (dd, 1H), 7.54 (d, 2H), 7.35 (d, 2H), 7.25 (td, 1H), 7.17 (dd, 1H) , 4.39 / 4.28 (2*d, 2H), 3.4 / 3.09 (2*m, 2H), 3.13 / 2.84 (2*m, 2H), 2.95 (m, 2H), 2.09 / 1.65 (2 *m, 2H), 1.86 / 1.36 (2*m, 2H), 1.6 (m, 2H), 1.09 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 469.1452 (469.1454) Elemental Analysis: C=56.19(56.35);H=5.57(5.80);N=5.97(5.97) PR: -12.560 (589nm, T=20°C, C=0.7) Intermediate 151: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(2-naphthalen-1-ylphenyl)methyl]-4-oxo-1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 151 is obtained from intermediates 129 and 228 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8 (m, 2H), 7.65-7.2 (m, 9H), 3.85 (m, 2H), 3.4 (m, 2H), 3.35-3 (2dd, 2H), 2.65 / 2.2 (2m, 2H), 2.5 / 2 (2m, 2H), 1.9-1.5 (m, 4H), 1.4 (2s, 18H), 1.35 (m, 2 H), 1.3 (2s, 9H), 1.1 (t, 3H), 0.65 (m, 2H) EXAMPLE 199: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[(2-naphthalen-1-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 199 is obtained from intermediate 151 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8 (m, 2H), 7.75-7.3 (m, 9H), 4.35-3.8 (2dd, 2H), 3.4 / 2.95 (2m, 2H), 3.2 / 2.7 (2m, 2H), 2.9 (m, 2H), 2.05 / 1.55 ​​(2m, 2H), 1.75 / 1.25 (2m, 2H), 1.5 (m, 2H), 1.2-0.7 (m , 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 467.2109 (467.2099) Elemental Analysis: C=66.50(66.94);H=6.26(6.70);N=6.08(6.00) PR: -25.420 (589nm, T=19°C, C=1.0) Intermediate 152: (3S)-3-{4-[Bis(tei"i-butoxycarboxy)amino]butyl}-1-[(2-tei"i-butylphenyl)methyl]-4-ethoxy-4-oxo-1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 152 is obtained from intermediate 129 and 2-tert-butylbenzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.6-7.15 (3m, 4H), 4 (m, 2H), 3.75 (dd, 2H), 3.45- 3.3 (m, 2H), 3 -2.75 (2m, 2H), 2.5 (dd, 2H), 2.4 (m, 2H), 2-1.85 (m, 2H), 1.4 (m, 2H), 1.4 (s, 18H) , 1.4 (t, 9H), 1.35 (s, 9H), 1.2 (t, 3H), 0.95-0.7 (m, 2H) EXAMPLE 200: (3S)-3-(4-Aminobutyl)-1-[(2-^-butylphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 200 is obtained from intermediate 152 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.57 / 7.46 (2m, 2H), 7.36 (m, 2H), 4.65 (AB, 2H), 3.68 / 3.41 (2m, 2H), 3.46 / 3.22 (2m, 2H), 2.89 (m, 2H), 2.25 / 1.75 (2m, 2H), 1.9 / 1.46 (2m, 2H), 1.56 (quint., 2H), 1.35 (s, 9H ), 1.13 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 397.2253 (397.2256) Elemental Analysis: C=61.19(60.59);H=8.40(8.39);N=7.29(7.07) PR: -41.120 (589nm, T=19°C, C=0.9) Intermediate 153: (3S)-3-{4-[Bis(ter^butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-fluoro-2-(4-fluoro-3-methoxyphenyl)phenyl]methyl tert-Butyl]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 153 is obtained from intermediates 129 and 273 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.51 (dd, 1H), 7.28 (dd, 1H), 7.21 (dt, 1H), 7.09 (m, 1H), 7.09 (m, 1 H), 6.93 (m, 1H), 3.93 (m, 2H), 3.88 (s, 3H), 3.52 / 3.35 (2*d, 2H), 3.4-3.25 (m, 2H), 2.72 / 2.21 (2*m, 2H), 2.72 / 2.34 (2*m, 2H), 1.9-1.65 (m, 2H), 1.9-1.65 (m, 2H), 1.41 / 1.33 (2*s , 27H), 1.38 (m, 2H), 1.18 (t, 3H), 0.7 (m, 2H) EXAMPLE 201: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(4-fluoro-3-methoxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 201 is obtained from intermediate 153 according to procedure D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.6 (dd, 1H), 7.25 (m, 2H), 7.15 (m, 2H), 6.95 (m, 1H), 4.4 / 4.3 (2 *d, 2H), 3.9 (s, 3H), 3.5-3.3 (m, 1H), 3.2-3.05 (m, 2H), 2.95 (m, 2H), 2.9 (dd, 1H) , 2.05 (m, 1H), 1.85 (m, 1H), 1.65 (m, 1H), 1.6 (m, 2H), 1.35 (m, 1H), 1.2-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 483.1854 (483.1855) Elemental Analysis: C=57.37(57.26);H=5.95(6.06);N=5.86(5.81) PR: -21.910 (589 nm, T=21°C, C=1.1) Intermediate 154: (3S)-3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(2-isoquinolin-4-ylphenyl)methyl]-4-oxo-1,4 tert-Butyl -azaphosphinane-3-carboxylate Intermediate 154 is obtained from intermediates 129 and 264 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.35 (d, 1H), 8.32 (d, 1H), 8.21 (m, 1H), 7.71 (m, 2H), 7.6 (2*d , 1H), 7.5 (2*t, 1H), 7.42 (t, 1H), 7.31 (m, 1H), 7.25 (m, 1H), 3.87 (m, 2H), 3.45-3.3 (m, 2H), 3.32 / 3.2 / 3.05 (m, 2H), 2.62 / 2.2 (m, 2H), 2.58 / 2 (m, 2H), 1.8-1.25 (m, 6H), 1.6 (m, 2H), 1.42 / 1.4 (2*s, 18H), 1.32 / 1.3 (2*s, 9H), 1.1 (m, 3H) NMR 31 P: (400 MHz, dmso-d6) δ ppm 44.94 EXAMPLE 202: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[(2-isoquinolin-4-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 202 is obtained from intermediate 154 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 9.3 (s, 1 H), 8.35 / 8 (2*s, 1 H), 8.2 (m, 1 H), 7.8-7.4 (m, 7 H), 4.4-3.8 (2AB, 2H), 3.6-3.2 / 3 (m, 2H), 3.1 / 2.7 (m, 2H), 2.91 (m, 2H), 2.1 / 1.55 ​​(m, 2 H), 1.75 / 1.25 (m, 2H), 1.6 (m, 2H), 1.15-0.75 (m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 25.29 ESI / FIA / HR and MS / MS: [M+H]+ = 468.2046 (468.2047) Elemental Analysis: C=64.83(64.23);H=5.86(6.47);N=9.17(8.99) Intermediate 155: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(2-methoxypyridin-4-yl)phenyl]methyl]- tert-Butyl 4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 155 is obtained from intermediates 129 and 244 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.2 (d, 1H), 7.5 (m, 1H), 7.45-7.3 (2m, 2H), 7.25 (m, 1H), 7 (dd , 1H), 6.8 (si, 1H), 3.9 (m, 2H), 3.9 (s, 3H), 3.6 / 3.35 (dd, 2H), 3.3 (m, 2H), 2.75 / 2.35 (dd, 2H), 2.7 / 2.25 (2m, 2H), 1.95 / 1.75 (2m, 2H), 1.75 (m, 2H), 1.4 (s, 18H), 1.35 (s, 9H) , 1.3 (m, 2H), 1.2 (t, 3H), 0.7-0.5 (m, 2H) EXAMPLE 203: (3S)-3-(4-aminobutyl)-4-hydroxy-1-[[ 2-(2-Methoxypyridin-4-yl)phenyl]methyl]-4-oxo-1,4-azaphosphinan-3-carboxylic Example 203 is obtained from intermediate 155 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.18 (d, 1 H), 7.65-7.35 (m, 4 H), 7.02 (d, 1 H), 6.85 (s, 1 H), 4.35 (dd, 2 H), 3.9 (s, 3H), 3.65-3 (m, 3H), 3-2.8 (m, 3H), 2.1 / 1.7 (2m, 2H), 1.85 / 1.35 (2m, 2H) , 1.6 (m, 2H), 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 448.1989 (448.2001) Elemental Analysis: C=59.15(59.05);H=6.25(6.76);N=9.64(9.39) PR: -11.440 (589nm, T=19.5°C, C=0.9) EXAMPLE 204: (3S)-3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[[2-(2-oxo-1H-pyridin-4-yl)phenyl]methyl]-1 acid, 4-azaphosphinane-3-carboxylic Example 204 is obtained from intermediate 155 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.65-7.3 (m, 4 H), 7.6 (d, 1 H), 6.55 (s, 1 H), 6.5 (d, 1 H), 4.35 (dd, 2 H), 3.5 (2m, 2H), 3.25 / 2.9 (2m, 2H), 2.9 (m, 2H), 2.15 / 1.7 (2m, 2H), 1.85 / 1.4 (2m, 2H), 1.6 (m, 2H), 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 434.1838 (434.1839) Elemental Analysis: C=58.88(58.19);H=6.31(6.51);N=9.95(9.69) PR: -10.530 (589nm, T=19°C, C=1.0) Intermediate 156: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-4-oxo-1-{2-[1-(tetr ahy dr o-2H- tert-butyl pyr an-2-yl)-1H-pyr azol-5-yl]benzyl}-1,4-azaphosphinan-3-carboxylate Intermediate 156 is obtained from intermediates 129 and 293 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.6 (d, 1H), 7.6-7.2 (m, 4H), 6.3 (d, 1H), 4.9-4.8 (dd, 1H), 4 -3.8 (m, 4H), 3.5-3.2 (m, 4H), 2.85-2.6 (m, 2H), 2.5-2.1 (m, 3H), 2-1.65 (m, 6H), 1.5 -1.25 (m, 5H), 1.4 (s, 18H), 1.35 (s, 9H), 1.2 (t, 3H), 0.85-0.6 (m, 2H) EXAMPLE 205: Acid (35)- 3-(4-aminobutyl)-4-hydroxy-4-oxo-1-[2-(1H-pyrazol-3-yl)benzyl]-1,4-azaphosphinane-3-carboxylic Example 205 is obtained from intermediate 156 according to procedure D previously described. 1H NMR: (300 / 400 / 500 MHz, dmso-d6) δ ppm 7.62 (d, 1H), 7.6 (d, 1H), 7.38 (t, 1H), 7.33 (d, 1H), 7.26 (t, 1H), 6.55 (d, 1H), 4.32 / 4.05 (dd, 2H), 3.59 / 3.19 (dd, 2H), 3.33 / 2.93 (dd, 2H), 2.74 (m, 2 H), 2.1 1 / 1.61 (2*m, 2H), 1.73 / 1.29 (2*m, 2H), 1.41 (m, 2H), 1.04 / 0.88 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 407.1843 (407.1848) Elemental Analysis: C=56.28(56.15);H=6.42(6.70);N=13.82(13.79) PR: -84.390 (589 nm, T=19°C, C=1.1) Intermediate 157: (35)-3-{4-[Bis(ieri-butoxycarbony])amino]buty]}-l-[[ tert-Butyl 2-(2-chlorophenyl)-4-fluorophenyl]methyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 157 is obtained from intermediates 129 and 253 according to procedure F previously described. 1H NMR: (300 / 400 MHz, dmso-d6) δ ppm 7.65-7.4 (m, 4H), 7.25 (m, 2H), 7 (m, 1H), 3.9 (m, 2H), 3.35 (d, 1H), 3.3 (m, 2H), 3.15 (d, 1H), 2.8-2.55 (m, 2H), 2.3 (m, 1H), 2.1 (m, 1H), 1.95 -1.7 (m, 4H), 1.45 (m, 2H), 1.45 / 1.35 (2*s, 27H), 1.15 (t, 3H), 0.75 (m, 2H) NMR 19 F: (300 / 400 MHz, dmso-d6) δ ppm -1 14.5 ESI / FIA / HR and MS / MS: [M+H]+ = 753.3436 (753.3441) EXAMPLE 206: Acid (3S)-3-(4-aminobutyl)-1-[[2-(2-chlorophenyl])- 4-Fluorophenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic Example 206 is obtained from intermediate 157 according to procedure D previously described. 1H NMR: (300 / 400 MHz, dmso-d6) δ ppm 7.7-7.35 (m, 4H), 7.35-7.2 (m, 2H), 7.1 (m, 1H), 4.1 (si, 2H) , 3.7-3 (m, 3H), 3-2.7 (m, 3H), 2.2-2 (m, 1H), 1.8 (m, 1H), 1.65 (m, 1H), 1.55 (m , 2H), 1.45-1 (m, 3H) ESI / FIA / HR and MS / MS: [M+H]+ = 469.1456 (469.1454) Elemental Analysis: C=56.86(56.35);H=5.21(5.80);N=5.91(5.97) PR_: -15.060 (589 nm, T=20°C, C= 1.0) Intermediate 158: (3S)-3-{4-[Bis(ter^butoxycarbonyl)amino]butyl}-1-[[2-(2,3-dimethoxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo- tert-Butyl 1,4-azaphosphinane-3-carboxylate Intermediate 158 is obtained from intermediate 129 and 2-(2,3-dimethoxyphenylbezaldehyde) according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.5 (m, 1H), 7.35-7.2 (2m, 2H), 7.1 (m, 1H), 7.05-7 (2m, 2H), 6.7 (dd, 1H), 3.9 (m, 2H), 3.85 (s, 3H), 3.45 (s, 3H), 3.4 (m, 2H), 3.35 (dd, 2H), 2.7 / 2.4 (2m, 2H), 2.65 / 2.2 (2m, 2H), 1.95-1.7 (m, 4H), 1.45 (s, 18H), 1.4 (m, 2H), 1.35 (s, 9H) , 1.2 (t, 3H), 0.9 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 761.4136 (761.4142) EXAMPLE 207: (3S)-3-(4-Aminobutyl)-1-[[2-(2,3-dimethoxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan-3-acid carboxylic Example 207 is obtained from intermediate 158 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.65-7.35 (m, 4H), 7.25 (m, 1H), 7.2 (m, 1H), 6.9-6.8 (2dd, 1H), 4.35-3.9 (2dd, 2H), 3.86 (s, 3H), 3.7-2.65 (m, 4H), 3.4-3.35 (2s, 3H), 2.9 (m, 2H), 2.5-1.6 (m, 4 H), 1.6 (m, 2H), 1.5-0.9 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 477.2149 (477.2154) Elemental Analysis: C=61.06(60.50);H=6.99(6.98);N=5.97(5.88) Intermediate 159: (3S)-3-{4-[Bis(tert-butoxycarbonyl)amino]butyl)-4-hydroxy-1-[[2-(2-methylsulfonylphenyl)phenyl]methyl]-4-oxo-1, tert-Butyl 4-azaphosphinane-3-carboxylate Intermediate 159 is obtained from intermediate 129 and 2-(2-methylsulfonylphenyl)benzaldehyde according to procedure F previously described. 1H NMR: (300 / 400 MHz, dmso-d6) δ ppm 8.1 (d, 1H), 7.8-7.65 (2*m, 2H), 7.55 (d, 1H), 7.45 (m, 1H) , 7.3 (d, 1H), 7.25 (d, 1H), 7.25 (m, 1H), 3.95 (m, 2H), 3.5-3.25 (m, 4H), 3.1 (dd, 1H), 2.9-2.6 (2*m, 2H), 2.85 (2*s, 3H), 2.45 (m, 1H), 2.3 (m, 1H), 2.1 (m, 1 H), 2- 1.65 (m, 4H), 1.5-1.3 (4s, 27H), 1.2 (m, 3H), 0.75 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 779.3696 (779.3701) EXAMPLE 208: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[[2-(2-methylsulfonylphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 208 is obtained from intermediate 159 according to procedure D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.2 (d, 1H), 7.9 / 7.8 (2*m, 2H), 7.8-7.4 (m, 4H), 7.55 (d, 1H) , 4.4-3.8 (4d, 2H), 3.8-3.5 (m, 1H), 3.5-2.85 (m, 5H), 3.1 / 3 (2*s, 3H), 2.4-1.85 (m, 2 H), 1.8 (m, 1H), 1.7 (m, 2H), 1.6-1.1 (m, 3H) ESI / FIA / HR and MS / MS: [M+H]+ = 495.1716 (495.1713) Elemental Analysis: C=55.39(55.86);H=5.77(6.32);N=5.61(5.66);S=6.24(6.48) Intermediate 160: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(2-naphthalen-2-ylphenyl)methyl]-4-oxo-1 tert-Butyl ,4-azaphosphinane-3-carboxylate Intermediate 160 is obtained from intermediates 129 and 240 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8-7.3 (m, 11H), 3.9 (m, 2H), 3.6 / 3.4 (dd, 2H), 3.3 (m, 2H), 2.75 / 2.3 (2dd, 2H), 2.7 / 2.2 (2m, 2H), 1.9 / 1.7 (2m, 2H), 1.75 (m, 2H), 1.4 (s, 18H), 1.3 (m, 2 H), 1.3 (s, 9H), 1.15 (t, 3H), 0.65 (m, 2H) EXAMPLE 209: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[(2-naphthalen-2-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 209 is obtained from intermediate 160 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 8-7.4 (m, 11 H), 4.35 (dd, 2 H), 3.35 / 3 (2m, 2 H), 3.1 / 2.7 (2dd, 2 H), 2.8 (m, 2H), 2 / 1.6 (2m, 2H), 1.75 / 1.2 (2m, 2H), 1.5 (m, 2H), 0.9 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 467.2095 (467.2099) Elementary Analysis: C=67.07(66.94);H=6.46(6.70);N=5.88(6.00) PR: -8.570 (589 nm, T=19°C, C=0.8) Intermediate 161: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-1-[[4-chloro-2-(4-fluorophenyl)phenyl]methyl]-4-ethoxy- tert-Butyl 4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 161 is obtained from intermediate 129 and 4-chloro-2-(4-fluorophenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.5 (d, 1H), 7.45 (dd, 1H), 7.4 (dd, 2H), 7.29 (t, 2H), 7.25 (d, 1 H), 3.92 (m, 2H), 3.5 / 3.3 (AB, 2H), 3.3 (m, 2H), 2.72 / 2.2 (2*m, 2H), 2.67 / 2.35 (2*m, 2 H), 2-1.7 (m, 2H), 1.8 (m, 2H), 1.4 (s, 18H), 1.35 (m, 2H), 1.32 (s, 9H), 1.18 (t, 3 H), 0.7 (m, 2H) NMR 31 P: (400 MHz, dmso-d6) δ ppm 44.88, -113.8 EXAMPLE 210: (3S)-3-(4-Aminobutyl)-1-[[4-chloro-2-(4-fluorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane- 3-carboxylic Example 210 is obtained from intermediate 161 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.57 (d, 1H), 7.51 (dd, 1H), 7.45 (d, 1H), 7.36 (m, 2H), 7.24 (t, 2H) , 4.4 / 4.27 (AB, 2H), 3.38 / 3.1 (m, 2H), 3.2 / 2.85 (m, 2H), 2.94 (m, 2H), 2.09 / 1.65 (m, 2H), 1.85 / 1.35 (m, 2 hrs), 1.59 (m, 2 hrs), 1.1 (m, 2 hrs) NMR 31 P: (400 MHz, D20) δ ppm 25.4, -110.5 ESI / FIA / HR and MS / MS: [M+H]+ = 469.1455 (469.1454) Elemental Analysis: C=56.27(56.35);H=5.43(5.80);N=5.97(5.97);C1=7.28(7.56) PR: -28.440 (589 nm, T=20°C, C=0.9) Intermediate 162: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-l- tert-Butyl [[4-fluoro-2-(4-hydroxyphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 162 is obtained from intermediates 129 and 265 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.6 (si, 1H), 7.49 (dd, 1H), 7.18 (d, 2H), 7.12 (td, 1H), 6.98 (dd, 1 H), 6.81 (d, 2H), 3.92 (m, 2H), 3.5 / 3.3 (AB, 2H), 3.3 (m, 2H), 2.72 / 2.2 (2*m, 2H), 2.67 / 2.35 (2*m, 2H), 2-1.7 (m, 2H), 1.8 (m, 2H), 1.4 (s, 18H), 1.35 (m, 2H), 1.32 (s, 9 H), 1.18 (t, 3H), 0.7 (m, 2H) NMR 31 P: (400 MHz, dmso-d6) δ ppm 45.1, -114.8 EXAMPLE 211: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(4-hydroxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane acid - 3-carboxylic Example 211 is obtained from intermediate 162 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.47 (dd, 1H), 7.12 (d, 2H), 7.09 (td, 1H), 7.01 (dd, 1H), 6.88 (d, 2H) , 4.3 / 4.16 (AB, 2H), 3.23 / 2.98 (m, 2H), 3 / 2.7 (m, 2H), 2.81 (m, 2H), 1.96 / 1.55 ​​(m, 2H), 1.72 / 1.21 (m, 2H), 1.49 (m, 2H), 0.95 (m, 2H) NMR 31 P: (400 MHz, D20) δ ppm 25.4, -113 ESI / FIA / HR and MS / MS: [M+H]+ = 451.1794 (451.1793) Elemental Analysis: C=58.16(58.66);H=5.71(6.27);N=6.30(6.22) PR: -16.520 (589 nm, T=20°C, C=0.9) Intermediate 163: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-l- tert-Butyl [4-fluoro-2-(1-methyl-1H-pyrazol-4-yl)benzyl]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 163 is obtained from intermediates 129 and 250 according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 8 (s, 1H), 7.7 (s, 1H), 7.4 (dd, 1H), 7.2 (dd, 1H), 7.05 (td, 1 H), 3.97 (m, 2H), 3.9 (s, 3H), 3.6 / 3.4 (dd, 2H), 3.25 (m, 2H), 3 / 2.35 (2m, 2H), 2.8 / 2.45 (2m, 2H), 2 (m, 2H), 1.8 (m, 2H), 1.4 (s, 18H), 1.35 (s, 9H), 1.3 (m, 2H), 1.2 (t , 3H), 0.65 (m, 2H) EXAMPLE 212: (3S)-3-(4-Aminobutyl)-1-[4-fluoro-2-(1-methyl-1H-pyrazol-4-yl)benzyl]-4-hydroxy-4-oxo-1-acid ,4-azaphosphinane-3-carboxylic acid Example 212 is obtained from intermediate 163 according to procedure D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.81 (s, 1H), 7.7 (s, 1H), 7.6 (dd, 1H), 7.2 (m, 2H), 4.45 (dd, 2H) , 3.95 (sec, 3hrs), 3.5 / 3.25 (2m, 2hrs), 3.3 / 3 (2m, 2hrs), 3 (m, 2hrs), 2.1 / 1.75 (2m, 2hrs), 1.9 / 1.4 (2m, 2H), 1.65 (m, 2H), 1.15 (m, 2H) NMR 19 F: (300 MHz, D20) δ ppm -110.5 ESI / FIA / HR and MS / MS: [M+H]+ = 439.1905 (439.1910) Elemental Analysis: C=54.79(54.79);H=6.05(6.44);N=12.61(12.78) PR: -18.620 (589nm, T=19°C, C=0.9) Intermediate 164: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-fluoro-2-thiophen-2-ylphenyl)methyl]-4 tert-butyl -oxo-1,4-azaphosphinane-3-carboxylate Intermediate 164 is obtained from intermediates 129 and 246 according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.66 (dd, 1H), 7.47 (dd, 1H), 7.31 (dd, 1H), 7.25 (dd, 1H), 7.2 (dd, 1 H), 7.16 (td, 1H), 3.97 (m, 2H), 3.63 / 3.4 (dd, 2H), 3.25 (m, 2H), 2.88 / 2.32 (2m, 2H), 2.79 / 2.42 (dd, 2H), 2.05-1.9 (m, 2H), 1.82 (m, 2H), 1.39 (s, 18H), 1.33 (s, 9H), 1.3 (m, 2H), 1.2 (t, 3H), 0.7-0.4 (2m, 2H) NMR 19 F: (300 MHz, dmso-d6) δ ppm -113.9 EXAMPLE 213: (3S)-3-(4-Aminobutyl)-1-[(4-fluoro-2-thiophen-2-ylphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan-3-acid - carboxylic Example 213 is obtained from intermediate 164 according to procedure D previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.65 (dd, 1H), 7.55 (dd, 1H), 7.29 (dd, 1H), 7.2 (td, 1H), 7.15 (m, 2 H), 4.5 (dd, 2H), 3.5 / 3.2 (2m, 2H), 3.3 / 2.9 (2m, 2H), 2.9 (m, 2H), 2.1 / 1.75 (2m, 2H), 1.85 / 1.4 (2m, 2H), 1.6 (m, 2H), 1.1 (m, 2H) NMR 19 F: (300 MHz, dmso-d6) δ ppm -110 ESI / FIA / HR and MS / MS: [M+H]+ = 441.1405 (441.1413) Elemental Analysis: C=54.66(54.54);H=5.90(5.95);N=6.35(6.36);S=7.27(7.28) PR: -13.110 (589 nm, T=19.5°C, C=0.7) Intermediate 165: (3S)-3-{4-Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-l-[(2 tert-butyl isoquinolin-5-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 165 is obtained from intermediates 129 and 216 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.4 (s, 1H), 8.45 (d, 1H), 8.2 (m, 1H), 7.75 (m, 1H), 7.65 (m, 1 H), 7.6-7.4 (m, 3H), 7.2 (m, 1H), 7.15 (2*d, 1H), 3.95-3.7 (m, 2H), 3.5-3 (m, 4H) , 3.5-3.3 (m, 2H), 2.7-2.4 (m, 2H), 2.2 (m, 1H), 2 (m, 1H), 1.85 (m, 1H), 1.8 (m, 2 H), 1.7-1.5 (m, 1H), 1.5-1.25 (4s, 27H), 1.1 (t, 3H), 0.75-0.5 (m, 2H) EXAMPLE 214: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[(2-isoquinolin-5-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 214 is obtained from intermediate 165 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 9.25 (s, 1 H), 8.3 (dd, 1 H), 8.2 (m, 1 H), 7.85-7.55 (m, 5 H), 7.35 (m, 1 H), 7.3 (d, 1H), 4.45-3.8 (4d, 2H), 3.65-3.05 (m, 2H), 3.05-2.8 (m, 3H), 2.7 (m, 1H), 2.1 (m, 1H), 1.75 (m, 1H), 1.7-1.5 (m, 3H), 1.35-0.6 (m, 3H) ESI / FIA / HR and MS / MS: [M+H]+ = 468.2051 (468.2047) Elemental Analysis: C=64.96(64.23);H=6.08(6.47);N=9.03(8.99) Intermediate 166: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-fluoro-2-naphthalen-2-ylphenyl)methyl]-4 tert-Butyl -oxo-1,4-azaphosphinane-3-carboxylate Intermediate 166 is obtained from intermediates 129 and 247 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8-7.9 (m, 3H), 7.9 (si, 1H), 7.6-7.5 (m, 4H), 7.25 (td, 1H), 7.15 (dd, 1H), 3.9 (m, 2H), 3.6 / 3.4 (dd, 2H), 3.3 (m, 2H), 2.75 / 2.3 (2m, 2H), 2.7 / 2.2 (2m, 2 H), 1.9 / 1.75 (2m, 2H), 1.75 (m, 2H), 1.4 (s, 18H), 1.3 (s, 9H), 1.3 (m, 2H), 1.15 (t, 3 H), 0.7 (m, 2 H) EXAMPLE 215: (35)-3-(4-Aminobutyl)-1-[(4-fluoro-2-naphthalen-2-ylphenyl)methyl]-4-hydroxy-4-acid -oxo-1,4-azaphosphinane-3-carboxylic Example 215 is obtained from intermediate 166 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.08 (d, 1H), 8 (m, 2H), 7.95 (d, 1H), 7.7 (dd, 1H), 7.65 (m, 2H) , 7.54 (dd, 1H), 7.3 (m, 1H), 7.3 (dd, 1H), 4.65-4.2 (m, 2H), 3.35 / 3.05 (2m, 2H), 3.05 / 2.8 (2m , 2H), 2.85 (m, 2H), 2 / 1.65 (2m, 2H), 1.85 / 1.35 (2m, 2H), 1.55 (m, 2H), 0.9 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 485.2002 (485.2005) Elemental Analysis: C=63.97(64.45);H=6.21(6.24);N=5.93(5.78) PR: -6.790 (589 nm, T=19°C, C=0.7) Intermediate 167: (3S)-3-{4-[Bis(ter^butyloxycarbonyl)amino]butyl}-l-[[2-(l-benzothiophen-2-yl)-4-fluorophenyl]methyl]-4-ethoxy tert-Butyl -4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 167 is obtained from intermediates 129 and 217 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.05 (d, 1H), 7.9 (d, 1H), 7.6 (s, 1H), 7.55 (dd, 1H), 7.4 (m, 2 H), 7.35 (d, 1H), 7.3 (m, 1H), 3.95 (m, 2H), 3.75 (d, 1H), 3.5 (d, 1H), 3.25 (m, 2H) , 2.95 (m, 1H), 2.8 (m, 1H), 2.45 (dd, 1H), 2.35 (m, 1H), 2.05-1.6 (m, 4H), 1.42 (m, 2H) , 1.4 (s, 18H), 1.35 (s, 9H), 1.2 (t, 3H), 0.65 (m, 1H), 0.55 (m, 1H) EXAMPLE 216: (3S)-3-(4-Aminobutyl)-1-[[2-(1-benzothiophen-2-yl)-4-fluorophenyl]methyl]-4-hydroxy-4-oxo-1,4-acid -azaphosphinane-3-carboxylic Example 216 is obtained from intermediate 167 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.95 / 7.9 (2*d, 2 H), 7.65 (m, 1 H), 7.45 (m, 2 H), 7.4 (s, 1 H), 7.3 (m , 2H), 4.55 / 4.4 (2*d, 2H), 3.6-3.4 (m, 1H), 3.25 (m, 1H), 3.15 (m, 1H), 2.9 (dd, 1H) , 2.85 (m, 2H), 2.1 (m, 1H), 1.85 (m, 1H), 1.65 (m, 1H), 1.6-0.85 (m, 5H) ESI / FIA / HR and MS / MS: [M+H]+ = 491.1565 (491.1564) Elemental Analysis: C=59.10(58.77);H=5.38(5.75);N=5.84(5.71);S=6.42(6.54) PR: 0.930 (589 nm, T=20.5°C, C=1.0) Intermediate 168: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]buty]}-4-ethoxy-1-[4-fluoro-2-(1-methyl]-1H-imidazol- tert-Butyl 5-yl)benzy]]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 168 is obtained from intermediates 129 and 248 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.75 (s, 1H), 7.56 (2d, 1H), 7.29 (2t, 1H), 7.15 (2d, 1H), 6.9 (s, 1 H), 3.95 (m, 2H), 3.5-3.25 (m, 4H), 3.4 (s, 3H), 2.9 / 2.2 (2m, 2H), 2.65 / 2.3 (2m, 2H), 1.95 / 1.85 (2m, 2H), 1.85 (m, 2H), 1.4 (m, 2H), 1.4 (2s, 18H), 1.35 (2s, 9H), 1.2 (t, 3H), 1.1 -0.65 (m, 2H) EXAMPLE 217: (3S)-3-(4-Aminobutyl)-1-[4-fluoro-2-(1-methyl-1H-imidazol-5-yl)benzyl]-4-hydroxy-4-oxo-1 acid ,4-azaphosphinane-3-carboxylic acid Example 217 is obtained from intermediate 168 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.8 (s, 1H), 7.68 (dd, 1H), 7.33 (td, 1H), 7.22 (dd, 1H), 7.1 (s, 1H) , 4.25 / 4.18 (AB, 2H), 3.6 / 3.2 (2m, 2H), 3.45 (s, 3H), 3.3 / 3 (2m, 2H), 2.95 (m, 2H), 2.12 / 1.71 (2m, 2H), 1.9 / 1.42 (2m, 2H), 1.6 (m, 2H), 1.3-1 (m, 2H) NMR 19 F: (400 MHz, D20) δ ppm -109.75 ESI / FIA / HR and MS / MS: [M+H]+ = 439.1905 (439.1905) Elemental Analysis: C=54.41(54.79);H=6.12(6.44);N=12.74(12.78) PR: -27.720 (589nm, T=20°C, C=0.7) Intermediate 169: (3S)-3-{4-[Bis(tert-butoxycarbonyl)amino]butyl}-l-[[4-chloro-2-(4-methylphenyl)phenyl]methyl]-4-ethoxy-4- tert-butyl oxo-1,4-azaphosphinane-3-carboxylate Intermediate 169 is obtained from intermediate 129 and 4-chloro-2-(4-methylphenyl)benzaldehyde according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.52 (d, 1H), 7.4 (dd, 1H), 7.25 (dd, 4H), 7.2 (d, 1H), 3.9 (m, 2 H), 3.5 / 2.8 (dd, 2H), 2.8 (m, 2H), 2.75 / 2.2 (2m, 2H), 2.65 / 2.3 (2dd, 2H), 2.35 (s, 3H), 1.95 / 1.8 (2m, 2H), 1.8 (m, 2H), 1.4 (s, 18H), 1.35 (m, 2H), 1.35 (s, 9H), 1.18 (t, 3H), 0.7 (m, 2 H) EXAMPLE 218: (3S)-3-(4-Aminobutyl)-1-[[4-chloro-2-(4-methylphenyl)phenyl]methyl]-4-hydroxy-4-oxo-acid l,4-azaphosphinane-3-carboxylic Example 218 is obtained from intermediate 169 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.58 (d, 1H), 7.5 (dd, 1H), 7.42 (d, 1H), 7.38 (d, 2H), 7.23 (d, 2H) , 4.4 / 4.25 (AB, 2H), 3.35 / 3.1 (2m, 2H), 3.2 / 2.81 (2m, 2H), 2.95 (m, 2H), 2.39 (s, 3H), 2.09 / 1.68 (2m, 2H), 1.85 / 1.35 (2m, 2H), 1.6 (m, 2H), 1.2-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 465.1707 (465.1704) Elemental Analysis: C=60.11(59.42);H=6.34(6.50);N=6.09(6.03) PR: -26.100 (589nm, T=20°C, C=0.3) Intermediate 170: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-1-[2-(1,2-dimethyl-1H-imidazol-5-yl)-4-fluorobenzyl tert-Butyl]-4-ethoxy-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 170 is obtained from intermediates 129 and 274 according to procedure F previously described. 1H NMR: (300 / 400 MHz, dmso-d6) δ ppm 7.55 (dd, 1H), 7.2 (m, 1H), 7 (d, 1H), 6.75 (s, 1H), 4.05-3.7 (m, 4H), 3.5-3.3 (2*d, 2H), 3.25 (s, 3H), 3-2.2 (m, 4H), 2.35 (s, 3H), 2-1.3 (m , 6H), 1.4 (3s, 27H), 1.25 (m, 3H), 0.85 (m, 2H) EXAMPLE 219: (3S)-3-(4-Aminobutyl)-1-[2-(1,2-dimethyl-1H-imidazol-5-yl)-4-fluorobenzyl]-4-hydroxy-4-oxo-acid 1,4-azaphosphinane-3-carboxylic Example 219 is obtained from intermediate 170 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.75 (dd, 1H), 7.55 (s, 1H), 7.5 (m, 1H), 7.3 (dd, 1H), 4.25 (s, 2H) , 3.55 (m, 1 hr), 3.45 (s, 3 hrs), 3.4 (m, 1 hr), 3.25 (m, 1 hr), 3.15 (dd, 1 hr), 2.95 (t, 2H), 2.65 (sec, 3H), 2.15 (m, 1H), 1.9 (m, 1H), 1.75 (m, 1H), 1.65 (m, 2H), 1.45 (m, 1H ), 1.3 (m, 1H), 1.15 (m, 1H) ESI / FIA / HR and MS / MS: [M+H]+ = 453.2058 (453.2061) Elemental Analysis: C=46.18(47.29);H=5.24(5.86);N=10.02(10.50) PR: -28.200 (589nm, T=20°C, C=1.0) Intermediate 171: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-fluoro-2-imidazo[1,2-a]pyridin- tert-Butyl 3-ylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 171 is obtained from intermediates 129 and 234 according to procedure F previously described. 1H NMR: (300 MHz, dmso-d6) δ ppm 7.9 (d, 1H), 7.65 (m, 2H), 7.65 (s, 1H), 7.35-7.2 (m, 3H), 6.9 (m, 1H), 3.9 (quad., 2H), 3.35 (t, 2H), 3.35 / 3.25 (2*d, 2H), 2.8-2.4 (m, 3H) , 2.4 (dd, 1H), 2.2 (m, 1H), 1.9-1.6 (m, 3H), 1.5-1.3 (m, 2H), 1.45 (s, 18H), 1.35 (s, 9 H), 1.15 (t, 3H), 1-0.75 (m, 2H) EXAMPLE 220: (3S)-3-(4-Aminobutyl)-1-[(4-fluoro-2-imidazo[1,2-a]pyridin-3-ylphenyl)methyl]-4-hydroxy-4-oxo acid - 1,4-azaphosphinane-3-carboxylic Example 220 is obtained from intermediate 171 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.05 (d, 1H), 7.75 (dd, 1H), 7.7 (d, 1H), 7.7 (s, 1H), 7.45 (m, 1H) , 7.4 (m, 1H), 7.3 (d, 1H), 7 (m, 1H), 4.6-4 (m, 2H), 3.45 (m, 1H), 3.05 (m, 2H) , 2.9 (m, 2 hrs), 2.8 (dd, 1 hr), 2.1 (m, 1 hr), 1.8 (m, 1 hr), 1.65 (m, 1 hr), 1.55 (m, 2 hrs), 1.3 (m, 1H), 0.95 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 475.1906 (475.1905) Elemental Analysis: C=58.69(58.22);H=5.71(5.95);N=11.94(11.81) PR: -27.190 (589nm, T=20°C, C=1.0) Intermediate 172: (3S)-3-{4-[Bis(terf-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-fluoro-2-(2-methoxypyridin-4-yl)phenyl]methyl tert-Butyl]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 172 is obtained from intermediates 129 and 249 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.23 ​​(d, 1H), 7.52 (dd, 1H), 7.26 (td, 1H), 7.1 1 (dd, 1H), 7.01 (dd, 1H), 6.85 (si, 1H), 3.94 (m, 2H), 3.9 (s, 3H), 3.53 / 3.34 (dd, 2H), 3.31 (m, 2H), 2.74 / 2.24 ( 2m, 2H), 2.68 / 2.37 (2dd, 2H), 1.93 / 1.75 (2m, 2H), 1.86-1.66 (m, 2H), 1.41 (s, 18H), 1.36 (m, 2H ), 1.35 (s, 9H), 1.19 (2m, 2H), 0.69 / 0.61 (t, 3H) EXAMPLE 221: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(2-methoxypyridin-4-yl)phenyl]methyl]-4-hydroxy-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 221 is obtained from intermediate 172 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.17 (d, 1H), 7.64 (dd, 1H), 7.29 (td, 1H), 7.17 (dd, 1H), 7.01 (dd, 1H) , 6.86 (s, 1H), 4.32 (dd, 2H), 3.9 (s, 3H), 3.45 / 3.07 (2m, 2H), 3.17 / 2.84 (2m, 2H), 2.9 (m, 2 H), 2.1 / 1.68 (2m, 2H), 1.85 / 1.35 (2m, 2H), 1.6 (m, 2H), 1.07 (m, 2H) ESI / FIA / HR and MS / MS: [M +H]+ = 466.1905 (466.1902) Elemental Analysis: C=56.79(56.77);H=6.15(6.28);N=8.94(9.03) PR: -9.530 (589nm, T=19°C, C=1.0) EXAMPLE 222: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(2-oxo-1H-pyridin-4-yl)phenyl]methyl]-4-hydroxy-4-acid oxo-1,4-azaphosphinane-3-carboxylic acid Example 222 is obtained from intermediate 172 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.64 (dd, 1H), 7.62 (d, 1H), 7.29 (td, 1H), 7.18 (dd, 1H), 6.57 (d, 1H) , 6.53 (dd, 1H), 4.3 (dd, 2H), 3.51 / 3.15 (2m, 2H), 3.24 / 2.95 (2m, 2H), 2.92 (m, 2H), 2.13 / 1.7 (2m , 2H), 1.86 / 1.38 (2m, 2H), 1.58 (m, 2H), 1.1 (m, 2H) NMR 19 F: (400 MHz, D20) δ ppm -109.6 ESI / FIA / HR and MS / MS: [M+H]+ = 452.1745 (452.1745) Elemental Analysis: C=56.06(55.87);H=5.96(6.03);N=9.21(9.31) PR: -10.270 (589nm, T=19°C, C=0.9) Intermediate 173: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-hydroxy-2-(4-methylphenyl)phenyl]methyl]- tert-Butyl 4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 173 is obtained from intermediates 129 and 266 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.4 (s, 1H), 7.2 (s, 4H), 7.2 (d, 1H), 6.75 (dd, 1H), 6.7 (t, 1 H), 6.55 (s, 1H), 3.95 (m, 2H), 3.4 (d, 1H), 3.25 (d, 1H), 2.8 (m, 3H), 2.7 (dd, 1H) , 2.35 (s, 3H), 2.25 (dd, 1H), 2.15 (m, 1H), 1.9 (m, 1H), 1.85-1.7 (m, 3H), 1.35 (2s, 18H) , 1.25 (m, 2H), 1.2 (t, 3H), 0.75 (m, 2H) EXAMPLE 223: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[[4-hydroxy-2-(4-methylphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane- 3-carboxylic Example 223 is obtained from intermediate 173 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.47 (d, 1H), 7.35 (d, 2H), 7.22 (d, 2H), 6.95 (dd, 1H), 6.83 (d, 1H) , 4.32 / 4.19 (AB, 2H), 3.32 / 3.05 (2m, 2H), 3.18 / 2.77 (2m, 2H), 2.95 (m, 2H), 2.38 (s, 3H), 2.09 / 1.68 (2m, 2H), 1.85 / 1.35 (2m, 2H), 1.6 (m, 2H), 1.2-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 447.2045 (447.2043) Elemental Analysis: C=62.20(61.87);H=6.77(7.00);N=6.19(6.27) PR: -32.320 (589nm, T=20°C, C=0.7) Intermediate 174: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[4-methoxy-2-(imidazo[1,2-α]pyridin- tert-Butyl 3-yl)benzyl]-4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 174 is obtained from intermediates 129 and 267 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.98 (d, 1H), 7.66 (d, 1H), 7.63 (d, 1H), 7.5 (s, 1H), 7.29 (t, 1 H), 7.1 (dd, 1H), 6.98 (d, 1H), 6.9 (t, 1H), 3.9 (m, 2H), 3.8 (s, 3H), 3.35 (m, 2H) , 3.35 / 3.19 (AB, 2H), 2.7 / 2.25 (m, 2H), 2.62 / 2.1 (m, 2H), 1.85 / 1.7 (m, 2H), 1.65 (m, 2H), 1.4 (s, 18 H), 1.35 (m, 2 H), 1.3 (s, 9 H), 1.15 (t, 3 H), 0.65 (m, 2 H) EXAMPLE 224: Acid (35)-3-(4 -aminobutyl)-4-hydroxy-1-[4-hydroxy-2-(imidazo[1,2-a]pyridin-3-yl)benzyl]-4-oxo-1,4-azaphosphinane-3-carboxylic Example 224 is obtained from intermediate 174 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8 (d, 1H), 7.67 (s, 1H), 7.65 (d, 1H), 7.59 (d, 1H), 7.42 (t, 1H) , 7.09 (dd, 1H), 6.99 (t, 1H), 6.96 (df, 1H), 4.15 (m, 2H), 3.4 / 3.02 (m, 2H), 3.02 / 2.72 (m, 2 H), 2.9 (m, 2H), 2.1 / 1.6 (m, 2H), 1.75 / 1.22 (m, 2H), 1.5 (m, 2H), 0.92 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 473.1950 (473.1948) Elemental Analysis: C=58.82(58.47);H=6.00(6.19);N=11.80(11.86) PR: -34.930 (589nm, T=18°C, C=0.9) Intermediate 175: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-methoxy-2-pyridin-4-ylphenyl)methyl]-4 tert-Butyl -oxo-1,4-azaphosphinane-3-carboxylate Intermediate 175 is obtained from intermediates 129 and 268 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 8.61 (d, 2H), 7.41 (d, 2H), 7.38 (d, 1H), 7 (dd, 1H), 6.8 (d, 1 H), 3.92 (m, 2H), 3.79 (s, 3H), 3.49 / 3.3 (AB, 2H), 2.73 / 2.18 (m, 2H), 2.73 (m, 2H), 2.67 / 2.3 (m, 2H), 1.95-1.8 (m, 2H), 1.7 (m, 2H), 1.35 (2s, 18H), 1.22 (m, 2H), 1.18 (t, 3H), 0.69 / 0.55 (m, 2H) EXAMPLE 225: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[(4-hydroxy-2-pyridin-4-ylphenyl)methyl]-4-oxo-1,4-azaphosphinan-3-acid -carboxylic Example 225 is obtained from intermediate 175 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 8.6 (d, 2H), 7.5 (d, 1H), 7.41 (d, 2H), 7.01 (dd, 1H), 6.88 (d, 1H) , 4.31 / 4.2 (AB, 2H), 3.41 / 3.05 (m, 2H), 3.15 / 2.8 (m, 2H), 2.97 (m, 2H), 2.09 / 1.65 (m, 2H), 1.85 / 1.35 (m, 2H), 1.6 (m, 2H), 1.09 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 434.1841 (434.1839) Elemental Analysis: C=58.51(58.19);H=5.87(6.51);N=9.77(9.69) PR: -28.730 (589nm, T=18°C, C=0.6) Intermediate 176: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[4-fluoro-2-(3-fluorophenyl)phenyl]methyl]- tert-Butyl 4-oxo-1,4-azaphosphinane-3-carboxylate Intermediate 176 is obtained from intermediates 129 and 269 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.52-7.08 (m, 7H), 3.92 (m, 2H), 3.51 / 3.32 (AB, 2H), 3.3 (m, 2H), 2.72 / 2.21 (m, 2 hrs), 2.69 / 2.36 (m, 2 hrs), 2-1.85 (m, 2 hrs), 1.78 (m, 2 hrs), 1.4 (s, 18 hrs), 1.34 (m, 2 H), 1.31 (s, 9H), 1.18 (m, 3H), 0.65 (t, 2H) NMR 19 F: (400 MHz, dmso-d6) δ ppm -112 / - 114 EXAMPLE 226: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(3-fluorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane- 3-carboxylic Example 226 is obtained from intermediate 176 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.65 (dd, 1 H), 7.5 (m, 1 H), 7.25 (m, 1 H), 7.25 (d, 1 H), 7.25-7.1 (m, 3 H), 4.4 (d, 1H), 4.3 (d, 1H), 3.5-3.35 (m, 1H), 3.2 (m, 1H), 3.15 (m, 1H), 2.95 (m, 2 H), 2.85 (dd, 1H), 2.1 (m, 1H), 1.85 (m, 1H), 1.7 (m, 1H), 1.6 (m, 2H), 1.35 (m, 1H) , 1.2-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 453.1748 (453.1749) Elemental Analysis: C=58.06(58.40);H=6.00(6.01);N=6.14(6.19) PR: -15.830 (589nm, T=20.5°C, C=1.0) Intermediate 177: (3S)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[(4-hydroxy-2-thiophen-2-ylphenyl)methyl]-4 -oxo-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 177 is obtained from intermediates 129 and 255 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.55 (s, 1H), 7.55 (d, 1H), 7.25 (d, 1H), 7.2 (d, 1H), 7.1 (m, 1 H), 6.8 (s, 1H), 6.75 (dd, 1H), 4 (m, 2H), 3.5 (d, 1H), 3.3 (d, 1H), 3.25 (m, 2H) , 2.95-2.8 (m, 2H), 2.4 (dd, 1H), 2.25 (m, 1H), 2.05-1.8 (m, 4H), 1.4 (s, 18H), 1.35 (s, 9 H), 1.3 (m, 2H), 1.2 (t, 3H), 0.65 (m, 2H) EXAMPLE 227: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[(4-hydroxy-2-thiophen-2-ylphenyl)methyl]-4-oxo-1,4-azaphosphinan-3-acid -carboxylic Example 227 is obtained from intermediate 177 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.55 (d, 1H), 7.45 (d, 1H), 7.2 (m, 1H), 7.15 (d, 1H), 6.95 (m, 2H) , 4.45 (d, 1H), 4.35 (d, 1H), 3.55-3.4 (m, 1H), 3.35-3.25 (m, 1H), 3.15 (m, 1H), 2.95 (m, 2 H), 2.9 (dd, 1H), 2.15 (m, 1H), 1.85 (m, 1H), 1.7 (m, 1H), 1.6 (m, 2H), 1.4 (m, 1H) , 1.2 (m, 1H), 1.1 (m, 1H) ESI / FIA / HR and MS / MS: [M+H]+ = 439.1450 (439.1451) Elemental Analysis: C=55.29(54.78);H=6.41(6.21);N=6.46(6.39);S=7.06(7.31) PR: -36.090 (589nm, T=20.5°C, C=1.0) Intermediate 178: (35)-3-{4-[Bis(tei"i-butoxycarbonyl)amino]butyl}-4-ethoxy-1-[[2-(4-fluorophenyl)-4-hydroxyphenyl]methyl]- 4-oxo-1,4-azaphosphinane- tert-Butyl 3-carboxylate Intermediate 178 is obtained from intermediates 129 and 270 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.5 (si, 1 H), 7.39 (dd, 1 H), 7.24 (dd, 1 H), 7.2 (d, 1 H), 6.75 (dd, 2 H), 6.6 (d, 2H), 3.92 (m, 2H), 3.31 / 3.21 (AB, 2H), 3.3 (m, 2H), 2.72 / 2.12 (2*m, 2H), 2.67 / 2.3 (2*m, 2H), 2-1.8 (m, 2H), 1.8 (m, 2H), 1.4 (s, 18H), 1.35 (m, 2H), 1.32 (s, 9 H), 1.18 (t, 3H), 0.7 (m, 2H). NMR 31 P: (400 MHz, dmso-d6) δ ppm -114.8 EXAMPLE 228: (3S)-3-(4-Aminobutyl)-1-[[2-(4-fluorophenyl)-4-hydroxyphenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane- 3-carboxylic Example 228 is obtained from intermediate 178 according to procedure D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.47 (d, 1H), 7.32 (dd, 2H), 7.22 (dd, 2H), 6.98 (dd, 1H), 6.85 (d, 1H) , 4.32 / 4.2 (AB, 2H), 3.37 / 3.05 (m, 2H), 3.15 / 2.8 (m, 2H), 2.95 (m, 2H), 2.09 / 1.65 (m, 2H), 1.85 / 1.35 (m, 2 hrs), 1.59 (m, 2 hrs), 1.1 (m, 2 hrs) NMR 19 F: (400 MHz, D20) δ ppm -113.5 ESI / FIA / HR and MS / MS: [M+H]+ = 451.1792 (451.1793) Elemental Analysis: C=58.29(58.66);H=6.12(6.27);N=6.20(6.22) PR: -36.630 (589nm, T=21°C, C=1.0) Intermediate 179: (3S)-3-{4-[Bis(ter^butoxycarbonyl)amino]butyl}-1-[[2-(3,4-dimethoxyphenyl)-4-hydroxyphenyl]methyl]-4-ethoxy- tert-Butyl 4-oxo-azaphosphinane-3-carboxylate Intermediate 179 is obtained from intermediates 129 and 256 according to procedure F previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 9.4 (m, 1 H), 7.2 (d, 1 H), 7 (d, 1 H), 6.85 (m, 2 H), 6.7 (dd, 1 H), 6.6 (dd, 1H), 3.95 (m, 2H), 3.8 (2s, 6H), 3.4 / 3.25 (2d, 2H), 3.3 (m, 2H), 2.8 (m, 1 H), 2.7 (m, 1H), 2.3 (dd, 1H), 2.15 (m, 1H), 1.9 (m, 1H), 1.8 (m, 3H), 1.4 / 1.25 (2m, 2 H), 1.4 (s, 18H), 1.35 (s, 9H), 1.2 (t, 3H), 0.75 (quint, 2H) EXAMPLE 229: (3S)-3-(4-Aminobutyl)-1-[[2-(3,4-dimethoxyphenyl)-4-hydroxyphenyl]methyl]-4-hydroxy-4-oxo-1,4-acid azaphosphinane-3-carboxylic Example 229 is obtained from intermediate 179 according to procedure D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.05 (s, 1H), 7-6.85 (dd;d, 2H), 6.85 (d, 1H), 6.25 (dd, 1H), 6.15 (s, 1H), 3.75 (s, 6H), 3.2 (d, 1H), 3.05 (d, 1H), 3-2.85 (m, 1H), 2.8-2.65 (m, 1H) , 2.45-2.25 (m, 3H), 2.15 (m, 1H), 1.85-1.7 (m, 2H), 1.65 (m, 1H), 1.3-1.15 (m, 3H), 0.9 (m , 1H), 0.8 (m, 1H) ESI / FIA / HR and MS / MS: ESI-HR + / -: [M+H]+ = 493.2098 (493.2098) Elemental Analysis: C=58.52(58.53);H=6.32(6.75);N=5.48(5.69) PR: -32.470 (589nm, T=20°C, C=0.9) EXAMPLE 230: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[(4-hydroxyphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 230 is obtained from intermediate 129 and 4-hydroxybenzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.32 (d, 2 H), 6.9 (d, 2 H), centered at 4.2 (AB, 2 H), 3.7 / 3.28 (2m, 2 H), 3.45 / 3.05 (2dd, 2H), 2.9 (m, 2H), 2.21 / 1.75 (2m, 2H), 1.9 / 1.45 (2m, 2H), 1.59 (m, 2H), 1.22 / 1.1 (2m, 2 H) ESI / FIA / HR and MS / MS: [M+H]+ = 357.1577 (357.1574) Elemental Analysis: C=54.12(53.93);H=6.96(7.07);N=7.93(7.86) PR: -56.580 (589 nm, T=20°C, C=1.0) EXAMPLE 231: (3S)-3-(4-Aminobutyl)-1-[[2-(4-chlorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid Example 231 is obtained from intermediate 129 and 2-(4-chlorophenyl)benzaldehyde according to procedures F and D previously described. NMR Ή: (300 MHz, D20) δ ppm 7.59 (m, 1H), 7.51 (m, 2H), 7.51 (d, 2H), 7.38 (m, 1H), 7.31 (d, 2H) , 4.33 (AB, 2H), 3.39 / 3.08 (2m, 2H), 3.15 / 2.83 (2m, 2H), 2.92 (m, 2H), 2.07 / 1.62 (2m, 2H), 1.83 / 1.34 (2m, 2H), 1.56 (m, 2H), 1.06 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 451.1541 (451.1553) Elemental Analysis: C=58.91(58.60);H=6.12(6.26);N=5.85(6.21) PR: -10.140 (589 nm.T=20°C.C=0.8) EXAMPLE 232: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[[2-[2-methyl-5-(trifluoromethyl)pyrazol-3-yl]phenyl]methyl]-4-oxo acid - 1,4-azaphosphinane-3-carboxylic acid Example 232 is obtained from intermediate 129 and 2-[1-methyl-3(trifluoromethyl)-1H-pyrazol-5-yl]benzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.63 / 7.46 (m, 4 H), 6.81 (s, 1 H), 4.21 (AB, 2 H), 3.65 (s, 3 H), 3.5 / 3.19 (2m , 2H), 3.26 / 3 (2m, 2H), 2.91 (m, 2H), 2.15 / 1.69 (2m, 2H), 1.87 / 1.4 (2m, 2H), 1.58 (m, 2H) , 1.11 (m, 2H) NMR 19 F: (300 MHz, D2Q δ ppm -61.8 ESI / FIA / HR and MS / MS: [M+H]+ = 489.1869 (489.1878) Elemental Analysis: C=51.64(51.64);H=6.03(5.78);N=11.47(11.47) PR: -27.030 (589 nm, T=20°C, C=0.9) EXAMPLE 233: Acid (3S)-3-(4-aminobutyl)-4-hydroxy-4-oxo-1-[[2- (trifluor omethyl)phenyl]methyl]-1,4-azaphosphinane-3-carboxylic acid Example 233 is obtained from intermediate 129 and 2-trifluoromethylbenzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.88-7.6 (m, 4H), 4.51 (AB, 2H), 3.69 / 3.43 (2m, 2H), 3.48 / 3.25 (2m, 2H), 2.92 (m, 2H), 2.22 / 1.78 (2m, 2H), 1.93 / 1.49 (2m, 2H), 1.59 (m, 2H), 1.23 / 1.09 (2m, 2H) NMR 19 F: (300 MHz, D20) δ ppm -58.3 ESI / FIA / HR and MS / MS: [M+H]+ = 409.1492 (409.1499) Elemental Analysis: C=49.52(50.00);H=5.85(5.92);N=7.00(6.86) PR: -38.120 (589 nm, T=20°C, C=1.0 EXAMPLE 234: (3S)-3-(4-Aminobutyl)-1-[(4-fluoro-2-pyrimidin-5-ylphenyl)methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan-3-acid - carboxylic Example 234 is obtained from intermediate 129 and 4-fluoro-(2-pyrimidinyl)benzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 9.2 (s, 1H), 8.82 (s, 2H), 7.7 (dd, 1H), 7.35 (td, 1H), 7.2 (dd, 1H) , 4.38 / 4.28 (2*d, 2H), 3.5 / 3.15 (2*m, 2H), 3.25 / 2.9 (2*m, 2H), 2.9 (t, 2H), 2.1 / 1.6 (2 *m, 2H), 1.85 / 1.6 (2*m, 2H), 1.6 / 1.1 (2*m, 2H), 1.38 / 1.1 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 437.1740 (437.1753) Elemental Analysis: C=54.96(55.04);H=4.82(6.00);N=12.78(12.84) PR: -23.070 (589 nm, T=20°C, C=1.1) EXAMPLE 235: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[[2-(2-methylpyrazol-3-yl)phenyl]methyl]-4-oxo-1,4-azaphosphinan- 3-carboxylic Example 235 is obtained from intermediates 129 and 280 according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.7-7.35 (m, 4H), 7.65 (d, 1H), 6.45 (d, 1H), 4.25 / 4.15 (dd, 2H), 3.6 (s, 3H), 3.5 / 3.2 (2m, 2H), 3.3 / 3 (dd, 2H), 2.9 (m, 2H), 2.15 / 1.7 (2m, 2 H), 1.9 / 1.4 (2m, 2H), 1.6 (m, 2H), 1.3-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 421.1998 (421.2004) Elemental Analysis: C=57.19(57.13);H=7.08(6.95);N=13.43(13.33) PR: -29.970 (589 nm, T=19.5°C, C=1.0) EXAMPLE 236: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(2-methylpyrazol-3-yl)phenyl]methyl]-4-hydroxy-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 236 is obtained from intermediates 129 and 277 according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.7 (dd, 1H), 7.65 (d, 1H), 7.39 (td, 1H), 7.24 (dd, 1H), 6.5 (d, 1H) , 4.25 / 4.13 (AB, 2H), 3.61 (s, 3H), 3.48 / 3.18 (m, 2H), 3.29 / 3 (m, 2H), 2.94 (m, 2H), 2.17 / 1.7 (m, 2H), 1.9 / 1.41 (m, 2H), 1.6 (m, 2H), 1.2 / 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 439.1903 (439.1905) Elemental Analysis: C=54.74(54.79);H=6.38(6.44);N=12.57(12.78) PR: -26.790 (589nm, T=21°C, C=1.0) EXAMPLE 237: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[(2-imidazo[1,2-a]pyridin-3-ylphenyl)methyl]-4-oxo-1,4-acid -azaphosphinane-3-carboxylic Example 237 is obtained from intermediates 129 and 227 according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.98 (d, 1H), 7.68 (s, 1H), 7.65 (d, 1H), 7.65 (m, 2H), 7.52 (m, 1H) , 7.45 (dd, 1H), 7.22 (m, 1H), 6.98 (t, 1H), 4.25 (m, 2H), 3.45 / 3.1 (2*m, 2H), 2.9 (m, 2 H), 2.85 (m, 2H), 2.12 / 1.55 ​​(2*m, 2H), 1.8 / 1.55 ​​(2*m, 2H), 1.55 / 0.95 (2*m, 2H), 1.28 / 0.95 (2*m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 457.1993 (457.1999) Elemental Analysis: C=60.73(60.52);H=6.00(6.40);N=12.29(12.27) PR: -33.550 (589 nm, T=19°C, C=0.9) EXAMPLE 238: Acid (3S)-3-(4-aminobutyl)-1-[[4-fluoro-2-(3-hydroxyphenyl)phenyl ]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic Example 238 is obtained from intermediates 129 and 254 according to procedures F and D previously described. 1H NMR: (400 MHz, dmso-d6) δ ppm 7.6 (dd, 1H), 7.4 (m, 1H), 7.25 (m, 1H), 7.15 (d, 1H), 6.95 (dd, 1 H), 6.9 (dd, 1H), 6.85 (s, 1H), 4.4 (d, 1H), 4.25 (d, 1H), 3.5-3.3 (m, 1H), 3.25-3 (m , 2H), 2.95 (m, 2H), 2.85 (dd, 1H), 2.1 (m, 1H), 1.85 (m, 1H), 1.65 (m, 1H), 1.6 (m, 2 H), 1.35 (m, 1H), 1.2-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 451.1794 (451.1793) Elemental Analysis: C=58.81(58.66);H=5.81(6.27);N=6.19(6.22) PR: -19.520 (589nm, T=21°C, C=1.0) EXAMPLE 239: (3S)-3-(4-Aminobutyl)-1-[[4-nuoro-2-(6-methoxypyridin-3-yl)phenyl]methyl]-4-hydroxy-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 239 is obtained from intermediate 129 and 4-fluoro-2-(6-methoxy-3-pyridinyl)benzaldehyde according to procedures F and D previously described. NMR Ή: (400 MHz, D20) δ ppm 8.1 (d, 1H), 7.8 (dd, 1H), 7.65 (dd, 1H), 7.3 (td, 1H), 7.15 (dd, 1H) , 7 (d, 1H), 4.4 / 4.3 (2d, 2H), 3.9 (s, 3H), 3.45 (m, 1H), 3.2 (dd, 1H), 3.1 (m, 1H), 2.95 (m, 2H), 2.85 (dd, 1H), 2.1 (m, 1H), 1.85 (m, 1H), 1.65 (m, 1H), 1.6 (m, 2H) ), 1.35 (m, 1H), 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 466.1903 (466.1902) Elemental Analysis: C=57.18(56.77);H=6.17(6.28);N=9.05(9.03) PR: -11.850 (589 nm, T=20°C, C=0.9 EXAMPLE 240: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[[2-(6-hydroxypyridin-3-yl)phenyl]methyl]-4-oxo-1,4-azaphosphinan- 3-carboxylic Example 240 is obtained from intermediate 129 and 2-(6-methoxy-3-pyridinyl)benzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.7 (dd, 1 H), 7.6 (d, 1 H), 7.55-7.4 (2 m, 4 H), 6.7 (d, 1 H), 4.4 (2 d coal, 2H), 3.5 (m, 1H), 3.3 (dd, 1H), 3.2 (m, 1H), 3 (dd, 1H), 2.95 (m, 2H), 2.1 (m, 1H), 1.9 (m, 1H), 1.7 (m, 1H), 1.6 (m, 2H), 1.4 (m, 1H), 1.1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 434.1840 (434.1839) Elemental Analysis: C=58.14(58.19);H=6.38(6.51);N=9.60(9.69) P_R_: -8.440 (589 nm, T=20°C, C=0.8) EXAMPLE 241: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(6-hydroxypyridin-3-yl)phenyl]methyl]-4-hydroxy-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 241 is obtained from intermediate 129 and 4-fluoro-2-(6-methoxy-3-pyridinyl)benzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.7 (dd, 1H), 7.6 (m, 2H), 7.3 (td, 1H), 7.2 (dd, 1H), 6.7 (d, 1H) , 4.35 (2 d coal, 2 H), 3.5 (m, 1 H), 3.25 (m, 1 H), 3.2 (m, 1 H), 3 (dd, 1 H), 2.95 (m, 2H), 2.1 (m, 1H), 1.9 (m, 1H), 1.7 (m, 1H), 1.6 (quint, 2H), 1.4 (m, 1H), 1.1 (m, 2H ) ESI / FIA / HR and MS / MS: [M+H]+ = 452.1746 (452.1745) Elemental Analysis: C=55.62(55.87);H=5.85(6.03);N=9.16(9.31) PR: -7.630 (589 nm, T=20°C, C=0.7) EXAMPLE 242: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[[4-hydroxy-2-(6-methoxypyridin-3-yl)phenyl]methyl]-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 242 is obtained from intermediates 129 and 230 according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.95 (d, 1H), 7.6 (dd, 1H), 7.4 (d, 1H), 6.9 (m, 2H), 6.7 (d, 1H) , 4.2-4.1 (2d., 2 hrs), 3.8 (s, 3 hrs), 3.3-2.95 (2 sts, 2 hrs), 3.1-2.7 (2 sts, 2 hrs), 2.85 (sts, 2 hrs), 2.0- 1.5 (2m, 2H), 1.75-1.25 (2m, 2H), 1.5 (m, 2H), 1.0 (m, 2H) Elemental Analysis: C=56.79(57.01);H=6.62(6.52);N=8.99(9.07) PR: -27.320 (589 nm, T=20°C, C=0.8) EXAMPLE 243: (3S)-3-(4-Aminobutyl)-4-hydroxy-4-oxo-1-[(2-oxo-1,3-dihydrobenzimidazol-5-y) acid ] )methyl]]-l,4-azaphosphinane-3-carboxylic acid Example 243 is obtained from Intermediate 129 and 2-oxo-1,3-dihydrobenzothiazole-5-carbaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.25 (s, 1 H), 7.2 (m, 2 H), 4.45 (d, 1 H), 4.25 (d, 1 H), 3.8-3.65 (m, 1 H), 3.55-3.4 (m, 1H), 3.35 (m, 1H), 3.1 (dd, 1H), 2.95 (m, 2H), 2.3-2.15 (m, 1H), 2-1.85 (m, 1H), 1.85-1.7 (m, 1H), 1.6 (m, 2H), 1.55-1.4 (m, 1H), 1.3-1 (m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 397.1635 (397.1635) EXAMPLE 244: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]methyl]-4-hydroxy-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 244 is obtained from intermediates 129 and 231 according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 8.2 (t, 1 H), 7.8 (dd, 1 H), 7.7 (dd, 1 H), 7.55 (m, 2 H), 7.2 (d, 1 H) , 4.7 (d, 1H), 4.5 (d, 1H), 4.2 (s (+m, 3H), 3.9 (m, 1H), 3.6 (m, 3H), 3.2 (t (+m , 2H), 2.6 (m, 1H), 2.05 (m, 2H), 1.8 (m, 2H), 1.7 (m, 1H), 1.4 / 1.3 (2m, 2H) NMR 19 F: (300 MHz, D20) δ ppm -110.9 ESI / FIA / HR and MS / MS: [M+H]+ = 466.1901 (466.1902) Elemental Analysis: C=57.09(56.77);H=6.16(6.28);N=8.87(9.03) PR: -69.790 (589 nm, T=19°C, C=0.8) EXAMPLE 245: (3S)-3-(4-Aminobutyl)-1-[[4-fluoro-2-(1,3-thiazol-2-yl)phenyl]methyl]-4-hydroxy-4-oxo-acid 1,4-azaphosphinane-3-carboxylic Example 245 is obtained from intermediates 129 and 232 according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 8 (d, 1H), 7.7 (m, 2H), 7.7 (dd, 1H), 7.3 (td, 1H), 4.5 (d, 1H) , 4.3 (d, 1H), 3.85 (m, 1H), 3.45 (m, 2H), 3.15 (dd, 1H), 2.9 (m, 2H), 2.3 (m, 1H), 1.85 (m, 2 hrs), 1.55 (m, 3 hrs), 1.2 (m, 1 hrs), 1 (m, 1 hrs) NMR 19 F: (300 MHz, D20) δ ppm -109 ESI / FIA / HR and MS / MS: [M+H]+ = 442.1358 (442.1360) Elemental Analysis: C=51.13(51.69);H=5.30(5.71);N=9.42(9.52);S=7.25(7.26) PR: -99.540 (589 nm, T=18°C, C=0.8) EXAMPLE 246: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[[4-hydroxy-2-(3-methylimidazol-4-yl)phenyl]methyl]-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic hydrobromide Example 246 is obtained from intermediates 129 and 276 according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 8.85 (s, 1H), 7.65 (d, 1H), 7.6 (s, 1H), 7.2 (dd, 1H), 7 (d, 1H) , 4.4 (m, 1H), 4.15 (m, 1H), 3.7 (m, 1H), 3.6 (s, 3H), 3.55-3.2 (2m, 2H), 3.1 (m, 1H ), 2.9 (m, 2H), 2.15 (m, 1H), 1.9 (m, 2H), 1.6 (m, 3H), 1.25 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 437.1947 (437.1948) Elemental Analysis: C=39.13(40.15);H=5.22(5.22);N=8.85(9.37) PR: -15.390 (589nm, T=21°C, C=1.0) EXAMPLE 247: (3S)-3-(4-Aminobutyl)-4-hydroxy-1-[[4-hydroxy-2-(2-methylpyrazol-3-yl)phenyl]methyl]-4-oxo-1 acid, 4-azaphosphinane-3-carboxylic Example 247 is obtained from intermediate 129 and 4-hydroxy-2-(2-methylpyrazol-3-yl)benzaldehyde according to procedures F and D previously described. 1H NMR: (400 MHz, D20) δ ppm 7.63 (s, 1H), 7.52 (dd, 1H), 7.08 (d, 1H), 6.9 (s, 1H), 6.44 (d, 1H) , 4.18 / 4.05 (2m, 2H), 3.61 (s, 3H), 3.45 / 3.15 (2m, 2H), 3.26 / 2.95 (2dd, 2H), 2.95 (m, 2H), 2.15 / 1.68 (2m, 2H), 1.9 / 1.4 (2m, 2H), 1.6 (m, 2H), 1.2 / 1.1 (2m, 2H) ESI / FIA / HR and MS / MS: [M+H]+ = 437.1947 (437.1948) Elemental Analysis: C=55.22(55.04);H=6.48(6.70);N=12.72(12.84) PR: -44.210 (589 nm, T=20°C, C=1.0) EXAMPLE 248: (3S)-3-(4-Aminobutyl)-1-[[2-(3,4-dimethoxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-1,4-azaphosphinan-3-acid carboxylic Example 248 is obtained from intermediate 129 and 2-(3,4-dimethoxyphenyl)benzaldehyde according to procedures F and D previously described. 1H NMR: (300 MHz, D20) δ ppm 7.6 (dd, 1H), 7.5 (m, 2H), 7.35 (dd, 1H), 7.1 (d, 1H), 7 (d, 1H) , 6.9 (dd, 1H), 4.45 / 4.3 (2d, 2H), 3.85 (2s, 6H), 3.35 / 3.1 (2 sts, 2H), 3.1 / 2.9 ...

Claims

DEMANDS 1. Compound of formula (I): in which Aki represents a Ci-C6 alkyl chain, X represents -(CH2) m -, -CH(R)-, -N(R)-, -CH2-N(R)-, -N(R)-CH2- or -CH2-N(R)-CH2-, m represents 0 or an integer from 1 to 4, R represents a hydrogen atom or a group chosen from alkyl Ci-C6, -Ak2-Ar l 5 - Ak2-Ari-Ar2 and -Ak2-Ari-0-Ar2, -Ak2-cycloalkyl or -Ak2-OH, Ak2 represents a linear or branched Ci-C6 alkyl chain, Ari and Ar2, whether identical or different, each represent an aryl or heteroaryl grouping. Ri and R2 each represent a hydrogen atom when X represents -(CH2) m -, - CH(R)-, -N(R)-, -CH2-N(R)- or -N(R)-CH2-, or together they form a bond when X represents -CH2-N(R)-CH2-, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl, Cy represents a group chosen from cycloalkyl, aryl, and heteroaryl. Ak3 represents a Ci-C3 alkyl chain, R4 and R5, whether identical or different, each represent a hydrogen atom or a fluorine atom, its optical isomers, and its addition salts to a pharmaceutically acceptable acid. A compound of formula (I) according to claim 1, wherein Ri, R2, R4 and R5 each represent a hydrogen atom, R3 represents NH2, X represents -N(R)-, -CH2-N(R)-, -N(R)-CH2- or -CH2-N(R)-CH2-, and R represents a group selected from -Ak2-Ari, -Ak2-Ari-Ar2 and -Ak2-Ari-O-Ar 2i where Ak2, Ari and Ar2 are as defined in claim 1. Compound of formula (la), special case of compounds of formula (I) according to claim 1: in which Ra represents a group chosen from -CH2-Ari and -CH2-Ari-Ar2, where Ari and Ar2 are as defined in claim 1. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-l-[[2-(3,4-dimethoxyphenyl)-4-fluorophenyl]methyl]-4-hydroxy-4-oxo-l,4-azaphosphinane-3-carboxylic acid, as well as its optical isomers and its addition salts to a pharmaceutically acceptable acid. Compound of formula (I) according to claim 1, which is (3S)-3-(4-aminobutyl)-l-[[4-fluoro-2-(4-methylphenyl)phenyl]methyl]-4-hydroxy-4-oxo-l,4-azaphosphinane-3-carboxylic acid, as well as its optical isomers and its addition salts to a pharmaceutically acceptable acid. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-l-[[4-fluoro-2-(4-methoxyphenyl)phenyl]methyl]-4-hydroxy-4-oxo-l,4-azaphosphinane-3-carboxylic acid, as well as its optical isomers and its addition salts to a pharmaceutically acceptable acid.

7. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-l-[[4-fluoro-2-(4-fluorophenyl)phenyl]methyl]-4-hydroxy-4-oxo-l,4-azaphosphinane-3-carboxylic acid, as well as its optical isomers and its addition salts to a pharmaceutically acceptable acid.

8. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-4-hydroxy-1-[(4-hydroxy-2-phenylphenyl)methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid, as well as its optical isomers and its addition salts to a pharmaceutically acceptable acid.

9. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-4-hydroxy-1-[2-(6-methoxypyridin-3-yl)benzyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid, together with its optical isomers and its addition salts to a pharmaceutically acceptable acid.

10. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-l-[[2-(4-chlorophenyl)-4-fluorophenyl]methyl]-4-hydroxy-4-oxo-l,4-azaphosphinane-3-carboxylic acid, as well as its optical isomers and its addition salts to a pharmaceutically acceptable acid.

11. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-l-[4-fluoro-2-(l-methyl-lH-imidazol-5-yl)benzyl]-4-hydroxy-4-oxo-l,4-azaphosphinane-3-carboxylic acid, as well as its optical isomers and its addition salts to a pharmaceutically acceptable acid.

12. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-l-[2-(l,2-dimethyl-lH-imidazol-5-yl)-4-fluorobenzyl]-4-hydroxy-4-oxo-1,4-azaphosphinane-3-carboxylic acid, together with its optical isomers and its addition salts to a pharmaceutically acceptable acid.

13. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-4-hydroxy-1-[[4-hydroxy-2-(4-methylphenyl)phenyl]methyl]-4-oxo-1,4-azaphosphinane-3-carboxylic acid, as well as its optical isomers and its acid addition salts pharmaceutically acceptable.

14. Compound of formula (I) according to claim 1, which is (35)-3-(4-aminobutyl)-4-hydroxy-l-[4-hydroxy-2-(imidazo[l,2-a]pyridin-3-yl)benzyl]-4-oxo-l,4-azaphosphinane-3-carboxylic acid, as well as its optical isomers and its addition salts to a pharmaceutically acceptable acid.

15. Pharmaceutical composition containing a compound of formula (I) according to any one of claims 1 to 14, in combination with one or more inert, non-toxic, pharmaceutically acceptable excipients or vehicles.

16. Pharmaceutical composition according to claim 15, characterized in that it further contains a fibrinolytic, an anticoagulant or an antiplatelet agent.

17. Compound according to any one of claims 1 to 14 intended for use as a TAFIa inhibitor.

18. Compound according to any one of claims 1 to 14 intended for use in the treatment, prevention or secondary prevention of strokes, myocardial infarction, angina pectoris, arteritis of the lower limbs, thromboses, in particular venous thromboses, pulmonary embolism, aortic aneurysms or dementias.

19. Compound according to any one of claims 1 to 14 intended to be used according to claim 17 or 18, in association with a fibrinolytic, an anticoagulant or an antiplatelet agent.

20. Compound according to any one of claims 1 to 14 intended to be used according to claim 19, in association with an injectable fibrinolytic selected from alteplase and tenecteplase.