135 results about "Oxazolidine E" patented technology

The present invention is directed to a new process of preparing highly pure Florfenicol. The invention is further directed to new oxazolidine derivatives useful in making Florfenicol and processes of making these derivatives. Examples of such intermediates include (4R,5R)-3-acetyl-2,2-dimethyl-4-hydroxymethyl-5-[4-(methylsulfonyl)phenyl]-1,3-oxazolidine; and (4S,5R)-3-acetyl-2,2-dimethyl-4-fluoromethyl-5-[4-(methylsulfonyl)phenyl]-1,3-oxazolidine.

The invention discloses a rivaroxaban intermediate, a structural formula of the rivaroxaban intermediate is represented by the following formula (III). The invention further discloses a preparation method for rivaroxaban. The method is characterized by: carrying out a cyclization reaction for 4-(4-isocyanatophenyl)-3-morpholinone and (R)-epichlorohydrin under a catalytic action of magnesium halide to generate (S)-4- morpholinonephenyloxazolidinone, followed by carrying out functional group conversion to obtain 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidine-3-yl] phenyl}-morpholine-3-ketone, then reacting with 5-chlorothiophene-2-formyl chloride to prepare the rivaroxaban. The preparation method provided by the present invention has advantages of mild reaction conditions, simple operation, high reaction yield and the like. In addition, the use of toxic and harmful reagents is avoided during the synthesis process, such that environmental pollution is reduced, and the method is applicable for the industrial production.

Solvent free, moisture curable reactive hot melt adhesives are prepared using an oxazolidine functional prepolymer and a polyfunctional isocyanate.

The invention relates to a method for preparing an oxazolidinone compound and an intermediate thereof. Specifically, two fragments are coupled to prepare the oxazolidinone compound by virtue of Suzuki reaction. The method is simple in process, short in reaction time and high in yield and is suitable for industrial production. Furthermore, the method for preparing the intermediate of the oxazolidinone compound has the advantages of simplicity in operation, high yield and low cost.

Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.

A process for the preparation of taxanes comprising

wherein R is a tert. butoxycarbonyl or benzoyl group; PMP is p-methoxyphenyl group; G₁ is acetyl group; G₂ is haloacetyl group comprising

• • a) protecting the C-7 hydroxyl group of 10-deacetylbaccatin III with haloacetyl chlorides and then acetylating the C-10 hydroxyl group with acetyl chloride to obtain a protected 10-deacetylbaccatin III (1);
  • b) subjecting the protected 10-deacetylbaccatin III (1) to coupling with an oxazolidine-5-caboxylic acid of formula 2

wherein R is tert. butoxycarbonyl or benzoyl; PMP is p-methoxyphenyl group in the presence of a condensation agent and an activating agent to obtain C-13 esters of formula 3;

c) treating the coupled products 3 with weak acidic medium to open the oxazolidine ring to obtain intermediates of formula 4;

wherein R is a tert. butoxycarbonyl or benzoyl group; G₁ is acetyl group; G₂ is haloacetyl group

d) subjecting the intermediates of compound 4 to selective deprotection of haloacyl group in the presence of acetyl group under mild alkaline condition at −20 to +40° C. for 6-24 h in the presence of ammonia or aliphatic amine or aromatic amines or their combination to obtain paclitaxel or docetaxel.

A method of selectively preparing a chiral 2S-amino alcohol useful in preparation of an amide sulfonated or acylated with alkyl, substituted aryl or substituted heteroaryl is described. The method involves reacting a di-tert-butyl diazene-1,2-dicarboxylate with a (4S)-4-benzyl-3-[(S)-trifluoromethyl-alkyl substituted alkanoyl]-1,3-oxazolidin-2-one to afford a di-tert-butyl 1-(1S,2S)-([(4S)-4-benzyl-2-oxo-1,3-oxazolidine-3-yl]-carbonyl}-trifluoromethyl-alkyl substituted alkyl)hydrazine-1,2-dicarboxylate. This dicarboxylate is then reduced to yield di-tert-butyl 1-(1S,2S)-[trifluoromethyl-alkyl substituted alkyl]hydrazine-1-(hydroxymethyl)-1,2-dicarboxylate. The resulting product is deblocked with an acid to yield the acid addition salt of (2S,3S)-trifluoro-hydrazino-methyl alkan-1-ol. The acid addition salt of (2S,3S)-trifluor-2-hydrazino-methyl alkan-1-ol is hydrogenated in the presence of a suitable metal catalyst to yield the amino alcohol (2S,3S)-2-amino-trifluoro-methyl alkan-1-ol HCl.

A method for tanning an animal substrate comprising the steps: i) agitating the animal substrate with a chromium-free tanning agent; and ii) agitating the animal substrate with a tanning agent having an oxazolidine group; wherein at least some of the agitation is performed in the presence of a solid particulate material having an average particle size of from 1 to 500 mm.

The present invention is directed to processes for the preparation of N-(3R, 3aS, 6aR)-hexahydrofuro[2,3-b]furan-3-yl-oxycarbonyl-, (4S,5R)-4-[4-(2-methylthiazolo-4-methyloxy)-benzyl]-5-i-butyl-[(3,4-methylenedioxyphenyl)sulfonyl]-aminomethyl-2,2-dimethyl-oxazolidine.

An improved method of preparing oxazolidine protected aminodiol compounds is disclosed. These compounds are useful intermediates in processes for making Florfenicol.

The invention discloses a preparation method of rivaroxaban, which includes the steps of 1) performing a one-step cyclization reaction to an intermediate, N-(4-aminophenyl)-2-(2-haloethyoxyl)acetamide, to prepare a key intermediate, 4-(4-aminophenyl)-3-morpholinone, of the rivaroxaban; 2) performing a series reactions comprising ring opening with an epoxide, a substitution reaction, a ring formation reaction and the like to the 4-(4-aminophenyl)-3-morpholinone to obtain an intermediate, 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidine-3-yl]phenyl}morpholine-3-one; and 3) performing a substitution reaction to the 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidine-3-yl]phenyl}morpholine-3-one with 2-chloroformyl-5-chlorothiophene to obtain the rivaroxaban. The whole preparation process is short in route, is high in yield, is less in pollution, can avoid usage of expensive metal palladium for nitroreduction and is suitable for industrial production.

The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C₁-C₄ alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C₁-C₄ alkanoylamido optionally substituted with a halogen atom or halogen atoms, C₁-C₄ alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C₁-C₄ alkyl or C₁-C₄ alkoxycarbonyl group, or the neighboring X and Y groups optionally form together with one or more identical or different additional hetero atom and —CH═ and/or —CH₂— groups an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably morpholine, pyrrole, pyrrolidine, oxo- or thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo- or thioxo-imidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo- or thioxo-oxazolidine, or 3-oxo-1,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C₁-C₄ alkyl, C₁-C₄ alkoxy, trifluoromethyl, hydroxy or optionally esterized carboxyl group, W is oxygen atom, as well as C₁-C₄ alkylene, C₂-C₄ alkenylene, aminocarbonyl, —NH—, —N(alkyl)-, —CH₂O—, —CH₂S—, —CH(OH)—, —OCH₂— group, wherein the meaning of alkyl is a C₁-C₄ alkyl group—, when the dotted bonds () represent simple C—C bonds then U is hydroxy group or hydrogen atom or when W is C₁-C₄ alkylene or C₂-C₄ alkenylene group, then one of the dotted bonds () can represent a further double C—C bond and in this case U means an electron pair, which participate in the double bond and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor. Furthermore objects of the present invention are the pharmaceutical compositions containing new benzoyl urea derivatives of formula (I) or optical antipodes or racemates or the salts thereof as active ingredients and processes for producing these compounds and pharmaceutical compositions.

The invention discloses a preparation method of high-purity 5-vinyl oxazolidine-2-thioketone. The preparation method comprises the following steps: carrying out coordination on 1-amino-3-butene-2-alcohol taken as a starting material by using lead nitrate water solution, carrying out annulation on the raw material and CS2 in alkaline environment of potassium hydroxide solution, filtering the reaction liquid, extracting the reaction liquid by using ethyl acetate, carrying out liquid separation, drying and rotary evaporation to obtain a crude product, purifying the water solution containing the crude product through a preparative liquid chromatograph, receiving a mobile phase in the retention time period of a target product, and carrying out rotary evaporation and drying to obtain the product. According to the method, the steps are simple, the operation is convenient, the cost is low and the output is relatively high; and according to the method, the single-pass preparation amount can be up to 0.2-0.3g and the purity is 99.0-99.5%.

Disclosed are a novel oxazolidinone derivative exhibiting inhibitory activity against CETP, a preparation method thereof, and a pharmaceutical composition comprising the same. Exhibiting excellent inhibitory activity against CETP, the oxazolidinone derivative can be effectively applied to the prevention or treatment of various CETP enzyme activity- or HDL cholesterol level-related diseases such as dyslipidemia, atherosclerosis, and coronary heart disease.