专利号:US-5468876-A 优先权日:1986-05-22 标题:Intermediates for the stereoconservative synthesis of 1-substituted (S)-and (R)-2-aminomethylpyrrolidines 发明人:FEDERSEL HANS-JUEGEN; HOE THOMAS; RAEMSBY STEN I; STROEM PETER H E 权利人:ASTRA AB 摘要:Disclosed are (R)- and (S)-isomers of the compounds of the Formulas II and III with at least 95% optical purity ##STR1## wherein R 1 and R 2 are the same or different and represent a hydrogen atom, a lower alkyl, lower alkenyl or lower alkynyl group, a cycloalkyl group or a group (CH 2 ) m Ph, wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group. n These compounds are intermediates in the stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines.
专利号:US-6013796-A 优先权日:1996-07-26 标 题:Preparation of naltrexone from codeine and 3-benzylmorphine 发明人:HUANG BAO-SHAN; LU YANSONG; JI BEN-YI; CHRISTODOULOU ARIS P 权利人:PENICK CORP 摘要:For the synthesis of 3-methylnaltrexone from codeine in this invention, codeine is converted to 6-acetylcodeine, which is N-demethylated to 6-acetylcodeine hydrochloride, followed by alkylating the nitrogen to form 17-cyclopropylmethylnorcodeine. The latter is oxidized to 17-cyclopropylmethylnorcodeinone. For the synthesis of naltrexone from morphine in this invention, morphine is converted to 3-benzylnormorphine as described above in the synthesis of noroxymorphone. 3-Benzylnormorphine is reacted with cyclopropylmethyl halide to produce 3-benzyl-17cyclopropylmethylnormorphine, a novel compound, which is oxidized to 3-benzyl-17-cyclopropylmethyl-normorphinone, a novel compound, by Swern oxidation.
专利号:US-8853401-B2 优先权日:2009-04-24 标 题 :Processes for the preparation of morphinane and morphinone compounds 发明人:HUDLICKY TOMAS; CARROLL ROBERT; LEISCH HANNES; MACHARA ALES; WERNER LUKAS; ADAMS DAVID R 权利人:HUDLICKY TOMAS; CARROLL ROBERT; LEISCH HANNES; MACHARA ALES; WERNER LUKAS; ADAMS DAVID R; UNIV BROCK 摘要:The present application describes processes for the synthesis of morphinane and morphinone compounds, useful as pharmaceutical agents. Also included are novel intermediates useful in the preparation of these compounds. The process comprises quaternization of oripavine to provide a mixture of the R- and S-isomeric (at the nitrogen) quaternary salts. The R-isomer is readily isolated and converted to various N-(R)-morphinane and N-(S)-morphinone compounds. The R-isomer, S-isomer or a mixture of R- and S-isomers may be demethylated and converted to various morphinane and morphinone compounds.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:EP-4613751-A1 优先权日:2024-03-07 标 题 :Method of making chemical compounds useful for the synthesis of buprenorphine
专利号:WO-8707271-A1 优先权日:1986-05-22 标 题 :A stereoconservative synthesis of 1-substituted (s)- and (r)-2-aminomethylpyrrolidines and intermediates thereto
摘要:Inoue, S.; Driess, M., Science of Synthesis Knowledge Updates, (2012) 4, 234. 摘要:Cuenca, A. B.; Fernández, E., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 1, 348.