专利号:US-7323575-B2 优先权日:2003-04-09 标题:Process for the synthesis of (2S)-indoline-2-carboxylic acid 发明人:SOUVIE JEAN-CLAUDE; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the synthesis of (2S)-indoline-2-carboxylic acid of formula (I): n nApplication in the synthesis of perindopril and its pharmaceutically acceptable salts.
专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:US-3944619-A 优先权日:1976-02-20 标 题 :Synthesis of d-2-amino-1-butanol 发明人:SINGH BALWANT 权利人:AMERICAN CYANAMID CO 摘要:D-2-Amino-1-butanol, for the synthesis of ethambutol hydrochloride, d,d'-2,2'-(ethylenediimino)di-1-butanol dihydrochloride, is produced in high purity and good yields by the reaction of butene-1, a nitrile, preferably an excess of acetonitrile, and chlorine to form N-[1-(chloromethyl)propyl]acetimidoyl chloride which is hydrolyzed to dl-2-amino-1-butanol, which can be isolated as the hydrochloride, or free base, or a mixture, resolved with L(+)- tartaric acid and the d-2-amino-1-butanol reacted with ethylene dichloride and then hydrochloric acid to form ethambutol hydrochloride. A minimum of by-products which are conveniently split out permits the economical synthesis of a pharmaceutical grade product.
专利号:US-6133018-A 优先权日:1997-06-02 标 题 :Enzymatic synthesis of chiral amines using -2-amino propane as amine donor 发明人:WU WEI; BHATIA MOHIT B; LEWIS CRAIG M; LANG WEI; WANG ALICE L; MATCHAM GEORGE W 权利人:CELGRO 摘要:2-Aminopropane is used as the amine donor in the stereoselective synthesis of a chiral amine from a ketone with a transaminase. In a typical embodiment, (S)-1-methoxy-2-aminopropane is prepared by bringing methoxyacetone into contact with a transaminase in the presence of 2-aminopropane as an amine donor until a substantial amount of methoxyacetone is converted to (S)-1-methoxy-2-aminopropane and 2-aminopropane is converted to acetone. In a second embodiment, L-alanine is prepared by bringing pyruvic acid into contact with a transaminase in the presence of 2-aminopropane as an amine donor.
专利号:EP-1075534-B8 优先权日:1998-03-11 标 题 :Improvements in the enzymatic synthesis of chiral amines 发明人:WU WEI; BHATIA MOHIT B; LEWIS CRAIG M; LANG WEI; WANG ALICE; MATCHAM GEORGE W 权利人:CELGRO 摘要:2-Aminopropane is used as the amine donor in the stereoselective synthesis of a chiral amine from a ketone with a transaminase. In a typical embodiment, (S)-1-methoxy-2-aminopropane is prepared by bringing methoxyacetone into contact with a transaminase in the presence of 2-aminopropane as an amine donor until a substantial amount of methoxyacetone is converted to (S)-1-methoxy-2-aminopropane and 2-aminopropane is converted to acetone. In a second embodiment, L-alanine is prepared by bringing pyruvic acid into contact with a transaminase in the presence of 2-aminopropane as an amine donor.
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