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    • 10. 发明申请
    • Process for the recovery of S -(+)-methyl- (2-chlorophenyl)- (6,7-dihydro- 4H-thieno [3,2-c] pyrid-5-yl) acetate hydrogen sulfate (clopidogrel bisulfate) from its (R) and mixture of (R) and (S)- isomers
    • 回收S - (+) - 甲基 - (2-氯苯基) - (6,7-二氢-4H-噻吩并[3,2-c]吡啶-5-基)乙酸乙酯硫酸氢盐(氯吡格雷硫酸氢盐)的方法 (R)和(R)和(S) - 异构体的混合物
    • US20050059696A1
    • 2005-03-17
    • US10842702
    • 2004-05-10
    • Manne ReddySajja EswaraiahAnumula ReddyAlla Sampath
    • Manne ReddySajja EswaraiahAnumula ReddyAlla Sampath
    • A61K31/4743C07D495/04C07D498/02
    • C07D495/04
    • A process for the recovery of compound of formula (I) where X represents hydrogen, fluoro, chloro, bromo or iodo atom, preferably 2-chloro which comprising the steps of f. preparing compound (−) or (±)-(2-chloro phenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate methyl ester hydrogen sulfate from its corresponding camphorsulfonic acid salt compound. g. transforming the obtained compound of step (a), into the compound of (2-chlorophenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetic acid. h. converting the compound of step (b) into racemic compound (±)-(2-chloro phenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate methyl ester hydrogen sulfate. i. resolving the obtained racemic compound of step (c), into the optically active (+)-(2-chloro phenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate methyl ester camphor sulfonic acid salt. j. further transforming the optically active (+) form compound of step (d) into their pharmaceutically acceptable salts.
    • 回收式(I)化合物的方法,其中X代表氢,氟,氯,溴或碘原子,优选2-氯,其包括以下步骤: 从其相应的樟脑磺酸制备化合物( - )或(±) - (2-氯苯基) - (6,7-二氢-4H-噻吩并[3,2-c]吡啶-5-基)乙酸甲酯硫酸氢盐 盐化合物。 G。 将得到的步骤(a)的化合物转化为(2-氯苯基) - (6,7-二氢-4H-噻吩并[3,2-c]吡啶-5-基)乙酸的化合物。 H。 将步骤(b)的化合物转化为外消旋化合物(±) - (2-氯苯基) - (6,7-二氢-4H-噻吩并[3,2-c]吡啶-5-基)乙酸甲酯硫酸氢盐 。 一世。 将得到的步骤(c)的外消旋化合物拆分成光学活性(+) - (2-氯苯基) - (6,7-二氢-4H-噻吩并[3,2-c]吡啶-5-基)乙酸乙酯 甲酯樟脑磺酸盐。 j。 进一步将步骤(d)的光学活性(+)形式化合物转化为其药学上可接受的盐。