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:WO-2023039068-A1 优先权日:2021-09-08 标题:Compositions and methods for synthesis of peptide nucleic acid intermediates 发明人:COULL JAMES M; GILDEA BRIAN D 权利人:NEUBASE THERAPEUTICS INC 摘要:The present disclosure provides intermediates for the synthesis of peptide nucleic acid (PNA) backbones and monomers, such as cyclic intermediates, and methods of making the same.
专利号:EP-1546135-B1 优先权日:2002-07-16 标题:Novel synthesis of irbesartan 发明人:NISNEVICH GENNADY; RUKHMAN IGOR; PERTSIKOV BORIS; KAFTANOV JULIA; DOLITZKY BEN-ZION 权利人:TEVA PHARMA 摘要:Provided is a novel synthesis of irbesartan employing a phase transfer catalyst. Also provided is irbesartan having a fine particle size.
专利号:US-7312340-B2 优先权日:2003-02-05 标 题:Synthesis of 2-butyl-3-(1-trityl-1H-tetrazol-5-YL)biphenyl-4-YL)-1,3-diazaspiro[4,4]- non-ene-4-one 发明人:DOLITZKY BEN-ZION; KAFTANOV JULIA; PERTSIKOV BORIS; RUKHMAN IGOR; NISNEVICH GENNADY 权利人:TEVA PHARMA 摘要:Provided is a novel method of making 2-butyl-3-[[2′(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.
专利号:US-10766921-B2 优先权日:2016-05-18 标 题 :Process and intermediates for the 6,7-alpha-epoxidation of steroid 4,6-dienes 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY 权利人:NZP UK LTD 摘要:The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.
专利号:WO-2005049586-A1 优先权日:2003-11-24 标 题:Process for production of (s) -n-pentanoyl-n-[[2’-(1h-tetrazole-5yl) [1,1’-biphenyl]-4-yl]methyl]-l-valine 发明人:CEPANEC IVICA; LITVIC MLADEN; KORETIC STEFANIJA; BARTOLINCIC ANAMARIJA; DRUSKOVIC VINKA; SPOREC ANITA 权利人:BELUPO LIJEKOVI KOZMETIKA D D; CEPANEC IVICA; LITVIC MLADEN; KORETIC STEFANIJA; BARTOLINCIC ANAMARIJA; DRUSKOVIC VINKA; SPOREC ANITA 摘要:The patent relates to a new process of synthesis of an antihypertensive agent, N-pentanoyl-N-[[2'-(1H-tetrazole-5-yl)[1,1'-biphenyl]-4-yl]methyl]-L-valine (1), also known under the generic name of valsartan, by selective reaction of N-pentanoyl-N-[[2'-(1H-tetrazole-5-yl) [1,1'-biphenyl]-4-yl]methyl]-L-valine methyl-ester (14) with metallic or quaternary ammonium trialkylsilanolates by SN2 reaction. The compound 14 was produced in four reaction steps starting from 2N-trityl-5-(4'-methylbiphenyl-2-yl)tetrazole (17) and L-valine methyl-ester (11). Free-radical bromination of the compound 17 with N-bromosuccinimide produced 2N-trityl-5-(4'-bromomethylbiphenyl-2-yl)tetrazole (7), which in the reaction with L-valine methyl-ester (11) results in N-[[2'-(2N-trityl-tetrazole-5-yl)[1,1'-biphenyl]-4Âyl]methyl]-L-valine methyl-ester hydrobromide (15). Acylation of the compound 15 with pentanoyl chloride in the presence of trialkylamine bases results in N-pentanoyl-N-[[2'-(2NÂtrityl-tetrazole-5-yl)[1,1'-biphenyl] -4-yl]methyl]-L-valine methyl-ester (16). Removal of trityl protecting group by strong acids produces the key intermediary, compound 14.