专利号:US-5075450-A 优先权日:1990-06-28 标 题 :Intermediates in the synthesis of 17β-acyl-3-carboxy-androsta-3,5-dienes 发明人:RASMUSSON GARY H; TOLMAN RICHARD L; PATEL GOOL F 权利人:MERCK & CO INC 摘要:New intermediates in the synthesis of 17β-acyl-3-carboxy-androsta-3,5-dienes, of the formula: ##STR1## wherein R 2 is 2-thiopyridyl, and n R 3 is C 2 -C 4 alkoxycarbonyl, C 1 -C 4 , or trifluoromethylsulfonyloxy. The above compounds are useful intermediates in producing testosterone 5α-reductase inhibitors which are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
专利号:US-2024327320-A1 优先权日:2023-02-06 标 题:Novel routes of chemical synthesis of 20s(oh)d3, 20s,25(oh)2d3, 20s,23s(oh)2d3, and 20s,23r(oh)2d3 and their modification of the immune activity of pbmcs 发明人:SLOMINSKI ANDRZEJ; BRZEMINSKI PAWEL; FABISIAK ADRIAN 权利人:UNITED STATE GOVERNMENT AS REPRESEN TED BY THE DEPT OF VETERANS AFFAIRS; UNIV OF WARSAW 摘要:The present disclosure is concerned with methods of making hydroxy derivatives of vitamin D3, compounds useful as intermediates in the preparation of the hydroxy derivatives, and methods of making the intermediates. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-6362009-B1 优先权日:1997-11-21 标 题 :Solid phase synthesis of heterocycles 发明人:MUNOZ BENITO; CHEN CHIXU 权利人:MERCK & CO INC 摘要:Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.
专利号:US-6340751-B1 优先权日:1998-07-24 标 题 :Process for the preparation of 4-substituted azetidinone derivatives 发明人:SAITO TAKAO; MURAYAMA TOSHIYUKI; MATSUMOTO TAKAJI; MIURA TAKASHI 权利人:TAKASAGO PERFUMERY CO LTD 摘要:Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): n and (IV): n represented by the following formula (III): n n n MgR 5 R 6   (III) n n n wherein R 5 represents a C 1-12 alkyl group, a C 2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C 1-4 alkyl group, a phenyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom, and R 6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR 7 group (R 7 representing a lower C 1-4 alkyl group, a substituted or unsubstituted phenyl group or a substituted or unsubstituted benzyl group). The process provides an industrially excellent process for the preparation of a 4-substituted azetidinone derivative which permits the selective preparation of an intermediate for the synthesis of a carbapenem antibacterial agent having a desired 1-β′ configuration.
专利号:US-2008207950-A1 优先权日:2004-12-22 标 题:Enantioselective Synthesis of a Sterically Hindered Amine 发明人:BERENS ULRICH; MALAN CHRISTOPHE; KIRNER HANS JURG 权利人:CIBA SC HOLDING AG 摘要:Compounds of the formula (I) wherein R is phenyl, or phenyl substituted by Cl, Br, C 1 -C 4 alkyl or CF 3 ; R 1 is H or methyl or ethyl; R 2 is H or methyl or acyl; R 3 is H or methyl; R′ 4 is —CH 3 or â•?CH 2 ; may be obtained in high enantiopurity by hydrogenation of a compound of the formula (II) wherein R and R 3 are as in formula (I); A is acyl; and R 4 is —CH 3 or â•?CH 2 ; in the presence of a chiral Rhodium or Ruthenium catalyst. Residues R 1 as methyl or ethyl and/or R 2 as H or methyl may subsequently be introduced without racemization by deacylation and optional alkylation.
专利号:US-2003092064-A1 优先权日:2001-04-05 标题 :System for the synthesis of spatially separated libraries of compounds and methods for the use thereof 发明人:READER JOHN C 权利人:MILLENNIUM PHARM INC 摘要:Featured is an apparatus useful for preparing combinatorial libraries of compounds in a parallel fashion so that the individual compounds of the library are spatially separate and the position of each compound of the library in the apparatus is known. Moreover, the apparatus is useful for the preparation of combinatorial libraries of compounds where the library is constructed from three or more building blocks, e.g., three, four, five, six or seven building blocks, resulting in a three, four, five, six or seven dimensional combinatorial library. Also featured are related methods for the preparation of three, four, five, six or seven dimensional combinatorial libraries of compounds using the apparatus of the present invention.