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US07754883B2 Method of racemization of the R(−) isomer of the (2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester 失效
（2-氯苯基）-6,7-二氢噻吩并[3,2-c]吡啶-5（4H） - 乙酸甲酯的R（ - ）异构体外消旋化方法

  • Patent Title: Method of racemization of the R(−) isomer of the (2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester
  • Patent Title (中): （2-氯苯基）-6,7-二氢噻吩并[3,2-c]吡啶-5（4H） - 乙酸甲酯的R（ - ）异构体外消旋化方法
  • Application No.: US11885654
    Application Date: 2006-03-03
  • Publication No.: US07754883B2
    Publication Date: 2010-07-13
  • Inventor: Josef Hajicek , Hana Stepankova , Jan Kalivoda
  • Applicant: Josef Hajicek , Hana Stepankova , Jan Kalivoda
  • Applicant Address: CZ Prague
  • Assignee: Zentiva k s
  • Current Assignee: Zentiva k s
  • Current Assignee Address: CZ Prague
  • Agency: Pearl Cohen Zedek Latzer, LLP
  • Priority: CZ2005-150 20050308
  • International Application: PCT/CZ2006/000010 WO 20060303
  • International Announcement: WO2006/094468 WO 20060914
  • Main IPC: C07D495/04
  • IPC: C07D495/04
Method of racemization of the R(−) isomer of the (2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester
Abstract:
Racemization of the R(−) isomer of the (2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester (Formula II) (also called R clopidogrel) is performed via conversion of a portion thereof to the S(+)isomer and it takes place in an organic solvent selected from alcohols, esters, ketones or ethers, or in their mixtures, in the presence of a base selected from substances of formula R1R2R3R4N+OH″ wherein R1, R2, R3 and R4 are identical or different substituents selected from C1-C5 alkyls or C5, C6 cycloalkyls or aryls, C7-C9 alkyl-cycloalkyls or alkyl-aryls, the molar ratio of the base to the starting substance being 1:1 to 1:10., OMe Cl I Cl
Abstract(Chinese):

（2-氯苯基）-6,7-二氢噻吩并[3,2-c]吡啶-5（4H） - 乙酸甲酯（式II）（也称为氯吡格雷）的R（ - ）异构体的外消旋化为 通过将其一部分转化成S（+）异构体而进行，并且其在选自醇，酯，酮或醚的有机溶剂或其混合物中，在选自式R 1 R 2 R 3 R 4 N + OH“，其中R 1，R 2，R 3和R 4是相同或不同的选自C 1 -C 5烷基或C 5，C 6环烷基或芳基的取代基，C 7 -C 9烷基 - 环烷基或烷基 - 芳基，碱与起始物质的摩尔比 为1：1至1:10，OMe Cl I Cl

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