专利号:US-4151205-A 优先权日:1975-01-27 标题 :Synthesis of vitamin E 发明人:COHEN NOAL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A synthesis of vitamin E in racemic or optically active forms from methacryolein or beta-hydroxyisobutyric acid including intermediates in this synthesis.
专利号:US-4051153-A 优先权日:1975-01-27 标题 :Intermediates in the synthesis of vitamin E 发明人:COHEN NOAL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A synthesis of vitamin E in racemic or optically active forms from methacryolein or beta-hydroxyisobutyric acid including intermediates in this synthesis.
专利号:US-5703223-A 优先权日:1994-09-02 标题 :Solid phase synthesis of oligonucleotides with stereospecific substituted phosphonate linkages by pentavalent grignard coupling 发明人:WICKSTROM ERIC; LE BEC CHRISTINE 权利人:UNIV JEFFERSON 摘要:The present invention provides a method for producing an oligonucleotide having stereospecific substituted phosphonate linkages by use of a pentavalent Grignard coupling reaction on a solid phase support. The method can be used for automated synthesis of oligonucleotides having sequential equatorial or axial stereospecific substituted phosphonate linkages.
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-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
摘要:Reissig, H.-U.; Zimmer, R., Science of Synthesis, (2008) 44, 328. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 643. 摘要:Jackowski, O.; Perez-Luna, A., Science of Synthesis Knowledge Updates, (2022) 3, 81. 摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 167. 摘要:Weibel, J.-M.; Blanc, A.; Pale, P., Science of Synthesis Knowledge Updates, (2018) 1, 19.