氯吡格雷关键中间体S-(+)-(2-噻吩乙胺基)(2-氯苯基)乙酸甲酯的合成研究(1)
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[摘要] 目的 研究氯吡格雷的中间体(S)-(+)-(2-噻吩乙胺基)(2-氯苯基)乙酸甲酯的合成。 方法 以(S)-邻氯苯甘氨酸甲酯的酒石酸盐、噻吩乙醇对甲苯磺酸酯等为原料，经中和、亲核取代反应合成目标化合物，考察溶剂、缚酸剂、原料比对产率的影响。 结果 目标化合物经1H-NMR、13C-NMR确证化学结构，确定了最佳实验条件为原料比(氨基酸酯∶磺酸酯)为2∶1、溶剂为乙腈、缚酸剂为磷酸氢二钾，产率达到80%，纯度高达99%。 结论 本研究为(S)-(+)-2-噻吩乙胺基-2-氯苯基乙酸甲酯的工业化生产提供了较为合理的工艺路线，也为氯吡格雷生产提供了合格的原料。
[关键词] (S)-(+)-(2-噻吩乙胺基)(2-氯苯基)乙酸甲酯；氯吡格雷；中间体；合成
[中图分类号] RQ463.5 [文献标识码] A [文章编号] 1673-7210(2012)08(a)-0024-02
Study on synthesis of key intermediate of Clopidogrel of S - (+) - Methyl - α - (2-Thienylethylamino) (2-Chlorophenyl) Aectate
WU Guizhen1 CHEN Renhong1 YE Lianbao2 OU Xiaomin2 TANG Xingsan1
1.Department of Food, Guangdong Food and Drug Vocational College, Guangdong Province, Guangzhou 510520, China; 2.Department of Pharmacy, College of Pharmacy, Guangdong Pharmaceutical University, Guangdong Province, Guangzhou 510006, China
[Abstract] Objective To study the synthesis of S - (+) - Methyl - α - (2-Thienylethylamino) (2-Chlorophenyl) Aectate. Methods S - (+) - Methyl - α - (2-Thienylethylamino) (2-Chlorophenyl) Aectate was synthesised by using (+) - Tartrate of Methyl (+) - α- Amino (2-chlorophenyl) Acetate and 2 - (2-Thienyl) Ethyl toluene – p - sulphonate as starting materials by neutrallzation reaction, nucleophilic substitution reaction and etc.. The effect of molar ratio of (+) - Tartrate of Methyl (+) - α- Amino (2-Chlorophenyl) Acetate to 2 - (2-Thienyl) Ethyl toluene – p - sulphonate, solvent and acid acceptor on the yield of S - (+) - Methyl - α -(2-Thienylethylamino) (2-Chlorophenyl) Acetate were investigated. Results The chemical structure of the target compound was confirmed by 1H-NMR, 13C NMR ......
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