CAS: 189028-95-3; (S)-3-((S)-5-(4-Fluorophenyl)-5-Hydroxypentanoyl)-4-Phenyloxazolidin-2-One

上下游产品

CAS号189028-93-1 (4S)-3-[5-(4-氟苯... | CAS号108-05-4 乙酸乙烯酯 | CAS号1246853-48-4 (R,S)-3-[5-(4-f... | CAS号67-63-0 异丙醇 | CAS号272778-12-8 3-[(2R,5S)-5-(4... | CAS号163222-33-1 依泽替米贝

(S)-4-苯基-2-恶唑烷酮置于硼烷二甲硫醚络合物,三甲基乙酰氯,三乙胺,(R)-2-甲基-Cbs-恶唑硼烷体系中,用 二氯甲烷 用作溶剂,化学反应 4.0H,反应生成(4S)-3-[(5S)-5-(4-氟苯基)-5-羟基戊酰基]-4-苯基-1,3-氧氮杂环戊烷-2-酮
参考文献:一种依折麦布关键中间体的异构体及其制备方法
标题:一种依折麦布关键中间体的异构体及其制备方法
摘要:本发明提供了如通式ⅰ所示的依折麦布的关键中间体的一种异构体(1S2R3R4S构型)及其制备方法.1S2R3R4S型异构体是依折麦布关键中间体(4S)‑3‑[(2R,5S)‑5‑(4‑氟苯基)‑2‑[(S)‑[(4‑氟苯基)氨基][4‑(三甲基硅氧基)苯基]甲基]‑1‑氧代‑(5‑三甲基硅氧基)戊基]‑4‑苯基‑2‑恶唑烷酮合成过程中的主要杂质之一.通过对1S2R3R4S型异构体的合成,为依折麦布关键中间体杂质检查,定量及定性分析提供了对照品,从而提高了依折麦布关键中间体的质量标准.

专利信息

专利号:US-8383810-B2
优先权日:2004-12-20
标题:Process for the synthesis of azetidinones
发明人：THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L
权利人:MERCK SHARP & DOHME; THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L
摘要:A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

专利号:US-6207822-B1
优先权日:1998-12-07
标 题:Process for the synthesis of azetidinones
发明人：THIRUVENGADAM TIRUVETTIPURAM K; FU XIAOYONG; TANN CHOU-HONG; MCALLISTER TIMOTHY L; CHIU JOHN S; COLON CESAR
权利人:SCHERING CORP
摘要:This invention provides a process for preparing the hypocholesterolemic compoundcomprising:(a) reacting p-fluorobenzoylbutyric acid with pivaloyl chloride and acylating the product with a chiral auxiliary to obtain a ketone of formula IV:(b) reducing the ketone of formula IV in the presence of a chiral catalyst to an alcohol:(c) reacting the chiral alcohol of step (b), an imine and a silyl protecting agent, then condensing the protected compounds to obtain a beta-(substituted-amino)amide of formula VII:(d) cyclizing the beta-(substituted-amino)amide of formula VII with a silylating agent and a fluoride ion catalyst to obtain a protected lactam of the formula VIII:and removing the protecting groups.The intermediates of formulas VII and VIII are also claimed.

专利号:US-2003204096-A1
优先权日:2002-03-25
标题 :Enantioselective synthesis of azetidinone intermediate compounds
发明人：FU XIAOYONG; MC ALLISTER TIMOTHY L; THIRUVENGADAM T K; TANN CHOU-HONG
权利人:SCHERING CORP
摘要:The application relates to a process for preparing a compound of Formula I n n n This compound is an intermediate used to produce compounds that are useful as hypocholesterolemic agents in the treatment and prevention of atheroschlerosis.

专利号:US-6627757-B2
优先权日:2001-03-28
标题 :Enantioselective synthesis of azetidinone intermediate compounds
发明人：FU XIAOYONG; MCALLISTER TIMOTHY L; THIRUVENGADAM T K; TANN CHOU-HONG
权利人:SCHERING CORP
摘要:The application relates to a process for preparing a compound of Formula IThis compound is an intermediate used to produce compounds that are useful as hypocholesterolemic agents in the treatment and prevention of atheroschlerosis.

专利号:US-2002193607-A1
优先权日:2001-03-28
标题:Enantioselective synthesis of azetidinone intermediate compounds

专利号:US-2006135755-A1
优先权日:2004-12-20
标题:Process for the synthesis of azetidinones