120202-69-9Relevant articles and documents
Method for recycling S - O-chloromandelic acid
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Paragraph 0032-0055, (2021/02/09)
The invention belongs to the technical field of chemical synthesis, and discloses a method for recycling S-o-chloromandelic acid. The o-chloromandelic acid is a clopidogrel hydrogen sulfate starting material. The method is characterized by comprising the following steps: concentrating a lipid solution of S-o-chloromandelic acid to dryness, and adding an alkaline aqueous solution to react at a hightemperature to racemize the S-o-chloromandelic acid; after the reaction is completed, adding a C2-C8 lipid solvent and adjusting the pH of the solution with an inorganic acid to be acidic; separatingan aqueous phase from an organic phase, and allowing the organic phase to be dried and directly reacted with a resolving agent to prepare R-o-chloromandelic acid. The invention provides a method forrecycling clopidogrel hydrogen sulfate intermediate waste, the influence of reaction byproducts on the environment is eliminated, the S-o-chloromandelic acid is converted and then used in the preparation process of clopidogrel hydrogen sulfate, and the economic value is very high.
RACEMIZATION PROCESS FOR THE PREPARATION OF AN INTERMEDIATE OF CLOPIDOGREL HYDROGEN SULPHATE
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Page/Page column 9-10, (2009/07/18)
The invention relates to a process for the preparation of the pharmaceutically applicable methyl (S)-(+)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)- acetate hydrogen sulphate (also known as S-(+)-clopidogrel hydrogen sulphate) of formula (I) comprising racemizing methyl (R)-(-)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine- 5(4H)-acetate or methyl (S)-(+)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)- acetate, or a mixture thereof in any proportion with a weak base in the presence of an organic solvent, converting the methyl (R,S)-(±)-α-(2-chlorophenyl)-6,7-dihydrothieno [3,2-c]pyridine-5(4H)-acetate of fomula (II) obtained to its sulphuric acid addition salt methyl (R,S)-(±)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetate hydrogen sulphate and converting it to methyl (S)-(+)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c] pyridine-5(4H)-acetate hydrogen sulphate of formula (I) by known manner.
PROCESS FOR PREPARING CLOPIDOGREL
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Page/Page column 13-14, (2008/12/07)
A process for the preparation of clopidogrel of formula (I) or its pharmaceutically acceptable salts, solvates, hydrates thereof is disclosed. The process comprises treating (+)-(S)-2-Chlorophenyl-(6,7-dihydro-4H-thieno[3,2- c]pyridin-5-yl)acetamide of formula (II) with acid to provide novel acid salt of (+)-(S)- 2-Chlorophenyl-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetamide of formula (III) wherein in S represent acid selected from hydrochloric acid, hydrobromic acid, phosphoric acid, benzoic acid, succinic acid, oxalic acid, malic acid, maleic acid, methanesulfonic acid, ethane sulfonic acid, benzenesulfonic acid, p-toluene sulfonic acid, nephthalene sulfonic acid and converting acid salt of (+)-(S)-2-Chlorophenyl- (6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetamide to Clopidogrel (I) and its pharmaceutically acceptable salts, hydrates, solvates thereof.