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297 results about "Phenethylamines" patented technology
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A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
Lactobacillus plantarum with function of reducing contents of biogenic amines in foods and application of lactobacillus plantarum
ActiveCN105132308AAcid resistantHas the ability to clearBacteriaMicroorganism based processesBiotechnologyFermentation
The invention belongs to the technical field of microorganisms and discloses lactobacillus plantarum with a function of reducing contents of biogenic amines in foods and application of the lactobacillus plantarum. The lactobacillus plantarum is resistant to acids and capable of strongly removing eight types of biogenic amines (including tryptamine, phenethylamine, putrescine, cadaverine, histamine, tyramine, spermidine and spermine) in vitro. After 1*1010CFU / ml of the lactobacillus plantarum and the eight types of biogenic amines are co-cultured for 24h, wherein the concentration of each type of the biogenic amines is 100mg / L, and the total amine concentration is 800mg / L, the total amine content is reduced by 70% approximately, the content of each type of the biogenic amines is reduced by 30%-100%, and the removal rate of histamine highest in toxicity is up to 96.69%. Further, the lactobacillus plantarum is capable of lowering pH to 4 in eight hours owing to quickness in acid generation, thereby having favorable fermentation potential. The lactobacillus plantarum is used for degradation of the biogenic amines in foods, especially in fermented foods and extensive in application prospect.
Owner:JIANGNAN UNIV
(S)-alpha-phenethylamine: pyruvate transaminase
Relating to an enzyme capable of efficiently converting a ketone compound to an optically active amino compound by transamination, and a process for preparing an optically active amino compound using the enzyme. An (S)-alpha-phenethylamine:pyruvate transaminase, which acts on (S)-alpha-phenethylamine and a ketone compound, thereby catalyzing transamination for forming acetophenone and an amino compound corresponding to the ketone compound; a process for preparing an optically active amino compound using the transaminase; and a method for culturing a microorganism for producing the above transaminase, comprising adding to a medium one or more compounds selected from the group consisting of propylamine, 1-butylamine, 2-butylamine, 2-pentylamine, isopropylamine and isobutylamine as an inducer for the enzyme when a microorganism for producing (S)-alpha-phenethylamine:pyruvate transaminase is cultured.
Owner:KANEKA CORP
Substituted phenethylamines with serotoninergic and/or norepinephrinergic activity
InactiveUS20080234257A1High crystallinityThe result is moreBiocideNervous disorderDiabetic retinopathyChemical synthesis
Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and / or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, attention deficit hyperactivity disorder, fibromyalgia, irritable bowel syndrome, and / or premature ejaculation are described.
Owner:ACADIA PHARMA INC
Novel use of chiral (R/S)-a-phenethylamine(+/-)-tartrate
InactiveCN101016311AGroup 4/14 element organic compoundsOrganic-compounds/hydrides/coordination-complexes catalystsCyanideTartrate
The invention discloses a making method of chiral (R / S)-a-phenethylamine (+ / -)-tartrate, which is reacted by R or S-patterned phenethylamine and (+) or (-) tartaric acid, wherein the chiral salt can be catalyst in the asymmetrical reaction with not less than 99%.
Owner:HEFEI UNIV OF TECH
Process for the preparation of dronedarone
InactiveUS7312345B2High yieldLow costBiocideCarbamic acid derivatives preparationAluminium chlorideAcetic anhydride
The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.
Owner:ISP INVESTMENTS LLC
Phenanthridine derivative as well as medicinal composition, preparation method and application thereof
The invention provides a phenanthridine compound with an effect of resisting hepatitis B and hepatitis C, a medicinal composition taking the same as an active medicine component, a preparation method and applications of the phenanthridine compound in preparing a medicine for resisting hepatitis C viruses, and preparing an anti-virus medicine. According to the invention, the activity of benzylphenethylamine alkaloid in resisting various viruses is discovered in a process of studying a plant anti-virus natural product, and an obvious effect in resisting viruses of hepatitis B and hepatitis C of a phenanthridine derivative is discovered through structure modification, structure-function relationship and structure optimization.
Owner:KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
Method for synthesizing bortezomib
The invention belongs to the field of synthesizing medicaments, and discloses a method for synthesizing bortezomib. In the method, 3-methyl butyraldehyde and R-(+)-1-phenylethylamine are used as initiative materials, and the [(1R)-3-methyl-1-[[(2S)-1-oxygen-3-phenyl-2[(pyrazine formyl) amino] propyl]amino]butyl]-boric acid is obtained by condensation, selective boric acid ester addition, hydrogenation deprotection, chiral condensation with L-phenylalanine, condensation with 2-carboxyl-piperazine and boric acidification. The synthesis method has the advantages of readily available raw materials, higher yield of the whole reaction route, mild reaction conditions, easy operation, lower production cost and the suitability for industrialized production.
Owner:CHANGZHOU YABANG PHARMA
Chiral zinc complex and copper complexes of alpha-phenylethylamine
InactiveCN102069014AGroup 4/14 element organic compoundsCarboxylic acid nitrile preparationBenzaldehyde4-chlorobenzaldehyde
The invention relates to a chiral zinc acetate complex of alpha-phenylethylamine, a chiral copper acetate complex of alpha-phenylethylamine and a chiral copper chloride complex of alpha-phenylethylamine which are used as catalyst. When the complexes are used in the nitrile silicification reactions of aromatic aldehydes such as benzaldehyde, 2-fluorobenzaldehyde, 2-methoxybenzaldehyde, 2-methylbenzaldehyde, 4-methylbenzaldehyde, 4-methoxybenzaldehyde, 4-fluorobenzaldehyde, 4-chlorobenzaldehyde and 4-bromobenzaldehyde to prepare chiral target products, the chiral catalysts have good catalytic activities and high enantioselectivity in the nitrile silicification reactions.
Owner:罗梅
Method for utilizing ultra-effective bonded phase chromatography to serially connect QDa while quickly detecting seven biogenic amines in white spirit
ActiveCN105866302AEasy to useEasy to operateComponent separationTesting beveragesBiogenic amineChromatography column
The invention discloses a method for utilizing an ultra-effective bonded phase chromatography to serially connect QDa while quickly detecting seven biogenic amines in white spirit and belongs to the technical field of detection. The method is characterized by the following steps: after extracting a to-be-detected wine sample with acetonitrile, taking BEH C18 bonded phase chromatographic column as a separating column and carbon dioxide (A)+ isopropanol (B) as flowing phase for performing gradient eluting, and adopting a QDa mass spectrometry detector for detecting after separating the sample through the ultra-effective bonded phase chromatography (UPC2). The method provided by the invention is simple, quick, accurate, reliable and applicable to the simultaneous detection for the contents of seven biogenic amines (histamine, putrescine, cadaverine, phenylethylamine, spermidine, tyramine and octopamine) in white spirit.
Owner:ANHUI GUJING DISTILLERY +1
Preparation method and application of glycopyrronium bromide chiral antipode
The invention belongs to the technical field of medicine, and discloses a preparation method of (3S,2'S), (3S,2'R), (3R,2'R) and (3R,2'S) four type chiral monomers of muscarine receptor antagonist racemic medicine glycopyrronium bromide. The method comprises the following steps: resolving racemic alpha-cyclopentylmandelic acid by a chemical resolution method by using L-Tyrosine methyl ester and (R)-alpha-phenylethylamine as resolution reagents to respectively prepare (S)-alpha-cyclopentylmandelic acid and (R)-alpha-cyclopentylmandelic acid; and carrying out esterification reaction to respectively obtain chiral intermediates (S) / (R)-alpha-cyclopentylmethyl mandelate. L / D-malic acid used as the raw material is subjected to four reaction steps, including condensation, carbonyl reduction, catalytic hydrogenation or transfer hydrogenation reduction debenzylation, and reduction alkylation or alkylogen alkylation, in a chiral synthesis mode to obtain another important chiral intermediate (S) / (R)-N-methyl-3-hydroxypyrrolidine. The chiral intermediate is subjected to ester exchange and quaterisation to respectively obtain the four (3S,2'S), (3S,2'R), (3R,2'R) and (3R,2'S) type glycopyrronium bromide chiral monomers. The result indicates that the (3R,2'S)-glycopyrronium bromide has the strongest cholinergic antagonistic action.
Owner:SHENYANG PHARMA UNIVERSITY +1
Optical active compound of 1-(3-benzoyloxy-propyl)-5-(2-(1-phenyl ethyl amine) propyl-7-cyano indoline as well as preparation method and application thereof
The invention provides an optical active compound of 1-(3-benzoyloxy-propyl)-5-(2-(1-phenyl ethyl amine) propyl-7-cyano indoline as well as a preparation method and the application thereof. The optical active compound is shown in a formula (1), comprises a (R,R) configuration and a (S,S) configuration and can be used as an intermediate for synthetizing silodosin. The optical active compound of the single formula (1) can be used for preparing an optical high-purity product and has good yield on the premise of ensuring good optical purity. The preparation method of the optical active compound uses low-cost chiral assistant agent of alpha-phenethylamine and derivatives thereof, has mild reaction conditions, low cost and controllable optical purity and is easy for industrialized production.
Owner:ZHEJIANG HUAHAI PHARMA CO LTD +1
Preparation method of sitagliptin intermediate
ActiveCN103755596AChiral raw materials are cheap and readily availableShort reaction pathCarbamic acid derivatives preparationOrganic compound preparationPhenethylaminesChemistry
The invention discloses a preparation method of a sitagliptin intermediate represented by formula 1. The preparation method comprises the following steps: step A, carrying out a reaction of beta-ketonic ester 2 with a chiral amine to obtain a chiral enamine 3, wherein the chiral amine is R(+)-alpha-phenylethylamine or D-(-)-phenylglycinol; step B, reducing the chiral enamine 3 to obtain a compound 4; step C, carrying out catalytic hydrogenation of the compound 4 to remove a chiral auxiliary group, and thus obtaining a compound 5; step D, protecting amino of the compound 5 by Boc to obtain a compound 6; and step E, hydrolyzing the compound 6 to obtain beta-amino acid 1. The method has the advantages of cheap and easily obtained chiral raw materials, short reaction route, simple operation, mild reaction conditions, no special requirements on equipment, high yield, low cost and small environment protection pressure, and has relatively good industrial application and economic value.
Owner:ZHEJIANG UNIV OF TECH
Intermediates of Sitagliptin and preparation method thereof
ActiveCN102126976ASimple processReduce dosageOrganic compound preparationAmino-carboxyl compound preparationSitagliptinChemical structure
The invention mainly relates to intermediates of Sitagliptin and a preparation method thereof. The intermediates of the Sitagliptin have chemical structures shown as II and III, wherein definitions of Ar, R1 and R2 are shown in the specifications. The compounds shown as the II and the III are prepared by reacting a compound shown as a formula I with a substituent of phenylethylamine, which serve as raw materials, under hydrogen pressure. The intermediates are used for synthetizing the Sitagliptin, so synthetic difficulty is reduced, purity of a product is improved, the using amount of a high-price catalyst is reduced, production cost is effectively reduced, and the intermediates and the method are suitable for industrialized production.
Owner:JIANGSU SENRAN CHEM +1
Synthesis process of palmatine and its salts
InactiveCN1733763ARaise quality standardsContent increased and stabilizedOrganic chemistryBenzeneAcetonitrile
The invention discloses a synthesis process of palmatine and its salts mainly comprising the following steps, (1) etherification, preparation of o-dimethoxybenzene, (2) acetonitrilizaiton, preparation of methylenedioxy benzene acetonitrile, (3) hydrogenization, preparation of o-dimethoxy-phenethylamine, (4) condensation, preparation of condensate hydrochlorates, (5) recondensation, preparation of palmatine, (6) preparation of corresponding salts from palmatine with related acids.
Owner:余娟
Formulation for enhanced delivery of phenethylamine
InactiveUS20070190187A1Promote absorptionTo promote metabolismBiocideOrganic chemistryPhenethylamineInternal medicine
The present invention is directed to a formulation comprising phenethylamine or a derivative thereof, and an MAO-B enzyme inhibitor. The present invention is also directed to a method of increasing the absorption of phenethylamine or a derivative thereof, into the bloodstream, cells and tissue. The method includes administering phenethylamine or a derivative thereof, in combination with an MAO-B enzyme inhibitor.
Owner:KNELLER BRUCE W +1
Process for producing optically active carboxylic acid
InactiveUS20110257401A1Produced inexpensively and efficientlyPreparation from carboxylic acid saltsOrganic compound preparationBlood Coagulation Factor XCyclohexene
It has been demanded to provide a process for industrially producing an intermediate for a compound that exhibits an inhibitory effect on activated blood coagulation factor X and is useful as a preventive and / or therapeutic agent for thrombotic diseases. The present invention provides a process for producing the (R)-α-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid, comprising reacting 3-cyclohexene-1-carboxylic acid and (R)-α-phenylethylamine using a mixed solvent of water and acetone or a mixed solvent of water and ethyl acetate as a solvent.
Owner:DAIICHI SANKYO CO LTD
Process for the preparation of substituted pyrrolidine derivatives and intermediates
ActiveUS20060128789A1Easy to operateHigh yieldBiocideOrganic chemistryCombinatorial chemistryPyrrolidine
Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4. A process for preparing camphor sultam is also provided.
Owner:BIOCRYST PHARM INC
Method for preparing (3R)-(-)-3-(2- acetamino)-5-methylhexanol
InactiveCN102898320AEmission reductionReduce manufacturing costOrganic compound preparationCarboxylic acid amides preparation1-phenylethanamineAlcohol
The invention provides a method for preparing an antiepileptic medicament pregabalin intermediate, i.e., (3R)-(-)-3-(2-acetamino)-5-methylhexanol. The method comprises the following steps of: salifying a (+ / -)-3-(2-acetamino)-5-methylhexanol racemic body serving as a raw material and (S)-(-)-1-phenylethylamine in a mixed solvent of alcohol and halogenated hydrocarbon, precipitating unnecessary S-shaped chiral isomer salts out, filtering, concentrating a filtrate, dissolving into water, and reacting by using an acid to obtain (3R)-(-)-3-(2- acetamino)-5-methylhexanol of which the e.e. value is 80-90 percent; and refining to obtain a (3R)-(-)-3-(2-acetamino)-5-methylhexanol product of which the e.e. value is 98-99 percent. The method has the advantages of high chiral monomer purity, wide reaction temperature range, convenience in operating and suitability for industrial production. The invention further provides a method for preparing a racemate, i.e., (+ / -)-3-(2-acetamino)-5-methylhexanol. The racemic body can be taken as a raw material for repeated use, so that the consumption of raw materials is lowered, environmental protection is promoted, and the method has high application value.
Owner:AURISCO PHARMACEUTICAL CO LTD
Triphosgene method for synthesizing benzene sulphanilamide, intermediate of glimepiride, drug for Type ii Diabetes Mellitus
The invention discloses a triphosgene method for synthesizing benzene sulphanilamide, the intermediate of glimepiride, a drug for Type ii Diabetes Mellitus. Triphosgene is slowly dropped into a solution which contains phenethylamine and 3-ethyl-4-methyl pyrroline ketone, at a controlled temperature, so that N-[2-(3-ethyl-4-methyl-2-oxidation-3-pyrroline-1-formylamino)ethyl]-benzene (3) is obtained; the product reacts with chlorosulfonic acid to generate sulfonated product; the sulfonated product reacts with ammonia water to generate crude product benzenesulfonamide; the crude product is refined through solvent treatment to generate fine product; the reaction formula is show in the specification. The triphosgene method is simple in technology, simple in operation and high in yield; compared with the conventional method of phosgene, the solid phosgene (triphosgene) method is safer and is convenient to operate.
Owner:姜树林
Phenacylamine derivatives, process for their production and pesticides containing them
InactiveUS7439366B2Effective controlImprove system performanceBiocideOrganic chemistryHalogenHydrogen
The present invention relates to a phenacylamine derivative of the formula (I) or a salt thereof:wherein A is alkyl, cycloalkyl, phenyl which may be substituted by Y, pyridyl which may be substituted by Y, or pyrazolyl which may be substituted by Y, R1 and R2 are each alkyl, or R1 and R2 may together form a 3- to 6-membered saturated carbocycle, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl or COR4, X is halogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkoxy, haloalkoxy, alkenyloxy, haloalkenyloxy, alkynyloxy, haloalkynyloxy, alkylthio, haloalkylthio, alkenylthio, haloalkenylthio, alkynylthio, haloalkynylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, dialkylaminosulfonyl, nitro, cyano, phenyl which may be substituted by Y, phenoxy which may be substituted by Y, benzyloxy which may be substituted by Y, or pyridyloxy which may be substituted by Y, and n is an integer of from 0 to 5.
Owner:ISHIHARA SANGYO KAISHA LTD
Method for full chemical synthesis of fibrauretin anti-bacterial anti-inflammatory medicine
The invention discloses a method for full chemical synthesis of a fibrauretin anti-bacterial anti-inflammatory medicine. The method adopts 3,4-dimethoxyphenylethylamine and 2,3-dimethoxybenzaldehyde as initial raw material, and prepares a target product by three-step chemical reaction including heat condensation, sodium borohydride reduction and cyclization reaction. The full chemical synthesis method of fibrauretin in the invention has the advantages of simple reaction steps, mild reaction conditions, low cost and high yield, and is suitable for industrial production.
Owner:广西中医学院
Bioproduction of phenethyl alcohol, aldehyde, acid, amine, and related compounds
Owner:NAT UNIV OF SINGAPORE
Deuterium free, stable isotope labeled 2-phenylethylamine hallucinogens and/or stimulants, methods of their preparation and their use
ActiveUS9435816B2Organic active ingredientsOrganic compound preparationStable Isotope LabelingStimulant
Deuterium free, stable isotope labeled hallucinogens and / or stimulants containing a 2-phenylethylamine-based structural unit and containing at least three stable isotopes selected from the group consisting of 13C, 15N and 18O as free bases and as their salts; method of their preparation and their use in the chemical analysis, in particular forensic chemical analysis, and in metabolic studies.
Owner:CHIRON CORP
Methods for sealing microcell containers with phenethylamine mixtures
A method for sealing a container having an opening by contacting the opening with a mixture including a phenethylamine and a first polymer, adding a fluid to be contained to the container, and then adding a second mixture, comprising a second polymer, whereupon an interaction between the first and second polymer mixtures result in a seal being formed over the opening, thereby containing the fluid. The first polymer is typically a water-swellable polymer and the second polymer is typically a hydrophilic polymer that will form an interpenetrating network with the swellable polymer.
Owner:E INK CORPORATION
Method for synthesizing capsaicin homolog
InactiveCN101973903ASimple preparation processRaw materials are easy to getOrganic compound preparationCarboxylic acid amides preparationPhenethylaminesChemical synthesis
The invention relates to a method for chemically synthesizing capsaicin homolog. The structure of capsaicin homolog is shown in the formula (1) in the specification, wherein R1 is alkyl, cycloalkyl or aryl with carbon atom number of 2-20; R2 is -H or -OCH3; and R3 is -H, -OCH3 or -OH. The method comprises the following steps: in the presence of an ammonium acetate catalyst, vanillin, 4-hydroxybenzaldehyde, 3-methoxylbenzaldehyde or 3,4-dimethoxybenzaldehyde reacts with excessive nitromethane in glacial acetic acid under the backflow state; the obtained 4-hydroxyl-3-methoxyl-beta-nitrostyrene, 4-hydroxyl-beta-nitrostyrene, 3-methoxyl-beta-nitrostyrene or 3,4-dimethoxyl-beta-nitrostyrene is reduced by a reducing agent and then is acidized; and the phenethylamine salt obtained through acidizing reacts with alkyl acyl chloride, thus obtaining capsaicin homolog. The method is simple and convenient in preparation process, easily obtained in raw materials and mild in reaction conditions and provides new development space for study of the capsaicin substances. The formula (1) is shown in the specification.
Owner:ZHEJIANG UNIV
Preparation method and application of dibenzylamine quaternary ammonium salt high-temperature-resistant acidizing corrosion inhibitor
ActiveCN109402639AGood dispersionImprove solubilityAmino compound purification/separationOrganic compound preparationEpoxyBenzene
Owner:SOUTHWEST PETROLEUM UNIV
Abuse deterrent and Anti-dose dumping pharmaceutical salts useful for the treatment of attention deficit/hyperactivity disorder
A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
Owner:PISGAH LAB
Method for preparing intermediate used for synthesizing bortezomib
ActiveCN103044467ARaw materials are cheap and easy to getEasy to operateGroup 3/13 element organic compoundsBoronic acidMethyl group
The invention discloses a method for preparing an intermediate used for synthesizing bortezomib, comprising the following steps of: carrying out an addition reaction on 3-methyl butyraldehyde and bis(pinacolaton)diboron, then carrying out sulfonylation or halogenating reaction, carrying out an amination reaction with R-(+)-1-phenylethylamine, carrying out catalytic hydrogenation a debenzylation reaction, and finally carrying out enantiomer resolution. Compared with the prior art, the preparation method of the R-(1-amino-3-methyl) butyl boronic acid pinacol cyclic ester intermediate, provided by the invention, has the advantages that raw materials are cheap and easy to get, operation is easy, reaction conditions are mild and optical purity is high, and especially post-processing is simple and the high-optical-purity bortezomib can be easily obtained without column chromatography separation when the intermediate prepared by the invention is used for synthesizing the bortezomib, so that industrial production requirement of the bortezomib is met and the preparation method provided by the invention has obvious effect and economic practicability.
Owner:重庆瑞泊莱制药有限公司
Compound containing structure of o-naphthaquinone and application
InactiveCN1660833AHigh speedImprove convenienceOrganic active ingredientsNervous disorderQuinoneHyperammonemic encephalopathy
A compound containing o-naphthalene quinone structure for preparing medicines to prevent and treat hyperammonemia and hepatic encephalopathy is prepared from natural Masonate F through structure reformation and optimization.
Owner:SUN YAT SEN UNIV
Nesting method for pregabalin intermediate mother liquor
ActiveCN103980144AEmission reductionSimple and fast operationOrganic compound preparationCarboxylic acid amides preparationPregabalinSolvent
The invention discloses a nesting method for a mother liquor of a free pregabalin intermediate (R)-(-)-3-(carbamyl methyl)-5-methylhexanol-(R)-(+)-alpha-phenethylamine salt. The method comprises the following steps: (1) feeding a phenethylamine salt (R)-(-)-3-(carbamyl methyl)-5-methylhexanol-(R)-(+)-alpha-phenethylamine salt to the mother liquor filtered by dissociation in the procedure, and adding a certain amount of solvent to agitate, heat and dissolve; (2) cooling, dropwise adding an acid to adjust the pH; (3) devitrifying at certain temperature, filtering, wherein the filtrate is the mother liquor, and baking the filter cake to obtain (R)-(-)-3-(carbamyl methyl)-5-methylhexanol. The atom utilization rate of the reaction is improved, environmental pollution caused by direct emission of the material in the mother liquor is avoided, the nesting method is mild in reaction condition, has no demands on special equipment and instrument and has green chemistry characteristics, and the production cost is greatly reduced.
Owner:ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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