专利号:US-9446995-B2 优先权日:2012-05-21 标 题:Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN-SOON; ILLINOIS INST OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-10189803-B2 优先权日:2008-02-22 标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-6013829-A 优先权日:1996-02-05 标 题 :Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl -3- phenyl propanoic acid, application to the synthesis of N-(mercaptoacyl) amino acid derivatives 发明人:DANVY DENIS; MONTEIL THIERRY; DUHAMEL PIERRE; DUHAMEL LUCETTE; LECOMTE JEANNE-MARIE; SCHWARTZ JEAN-CHARLES; NOEL-LEFEBVRE NADINE; GROS CLAUDE; PLAQUEVENT JEAN-CHRISTOPHE 权利人:BIOPROJET SOC CIV 摘要:PCT No. PCT/FR97/00218 Sec. 371 Date Nov. 26, 1997 Sec. 102(e) Date Nov. 26, 1997 PCT Filed Feb. 4, 1997 PCT Pub. No. WO97/29086 PCT Pub. Date Aug. 14, 1997Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl-3-phenylpropanoic acid of formula (I): characterized in that it comprises the steps consisting in: a) preparing the diol (VI) by reduction of a malonic ester (V) in the presence of a hydride; b) preparing the monoacetates (VII R) or (VII S) respectively; c) subjecting these monoacetates to an oxidation in order to form the acids (IX S) or (IX R); d) saponifying the compounds (IX S) or (IX R) in order to form the hydroxy acids (X S) or (X R); e) thioacylating the hydroxy acids (X S) or (X R) with a mercapto acid R1SH (XI), according to a Mitsunobu-type reaction, in order to lead to the desired acids (I R) (I S) respectively and application to the synthesis of N-(mercaptoacyl)amino acid derivatives (II).
专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-11891351-B2 优先权日:2020-03-20 标 题 :Synthesis of capsaicin derivatives 发明人:LAGER ERIK 权利人:AXICHEM AS 摘要:The present invention relates to the synthesis of capsaicin derivatives, specifically to the synthesis of 6-heptyne derivatives of capsaicin.
专利号:US-2007259917-A1 优先权日:2006-04-24 标题 :Processes for the synthesis of 3-isobutylglutaric acid 发明人:KANSAL VINOD K; CHAURASIA BRIJNATH P; PATEL HITESH K; SHELKE SHIVAJI H; MORE YOGESH P 权利人:KANSAL VINOD K; CHAURASIA BRIJNATH P; PATEL HITESH K; SHELKE SHIVAJI H; MORE YOGESH P 摘要:Provided are processes for the synthesis of 3-isobutylglutaric acid, an intermediate in the synthesis of (S)-Pregabalin.
参考文献:10.1107/s1600536811016370 摘要:Vasin VA, Bolusheva IY, Neverov VA, Somov NV. Methyl c-1-cyano-t-2-methyl-sulfonyl-3-phenyl-cyclo-propane-carboxyl-ate. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1504. 参考文献:10.1007/s10895-011-0915-2 摘要:Patil SR, Shelar DP, Rote RV, Jachak MN. A fluorescence study of new angular polycyclic blue light-emitting pyrazolo[3,4-h][1,6]naphthyridine and their interaction with bovine serum albumin (BSA). J Fluoresc. 2011 Nov;21(6):2037–52. doi: 10.1007/s10895-011-0915-2. 参考文献:10.1016/j.bmc.2011.06.054 摘要:Serafin K, Mazur P, Bak A, Laine E, Tchertanov L, Mouscadet JF, Polanski J. Ethyl malonate amides: a diketo acid offspring fragment for HIV integrase inhibition. Bioorg Med Chem. 2011 Aug 15;19(16):5000–5. doi: 10.1016/j.bmc.2011.06.054.