| (+)-氯吡格雷的合成工艺改进 |
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| 引用本文： | 梁美好,沈正荣. (+)-氯吡格雷的合成工艺改进[J]. 中国药物化学杂志, 2007, 17(3): 163-165 |
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| 作者姓名： | 梁美好 沈正荣 |
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| 作者单位： | 浙江省医学科学院,药物研究所,浙江,杭州,310013 |
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| 摘 要： | 目的改进抗血栓药物氯吡格雷硫酸氢盐的合成工艺。方法以(±)-邻氯苯甘氨酸为原料,经拆分、酯化,得到( )-邻氯苯甘氨酸甲酯,再与2-(2-噻吩基)乙醇对甲苯磺酸酯经SN2取代,生成α-2-噻吩乙氨基-2-氯苯基乙酸甲酯,后者在甲醛存在下环合制得( )-氯吡格雷游离碱,最后与硫酸成盐,经重结晶得目标产物氯吡格雷硫酸氢盐。结果与结论以26.9%的收率合成了目标产物,较大幅度地降低了生产成本,优化了反应条件,简化了后处理过程,适合于工业化生产。
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| 关 键 词： | 氯吡格雷 手性拆分 (±)-邻氯苯甘氨酸 抗血小板聚集抑制剂 |
| 文章编号： | 1005-0108（2007）03-0163-03 |
| 修稿时间： | 2006-12-18 |
Improved synthesis of clopidogrel |
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| LIANG Mei-hao,SHEN Zheng-rong. Improved synthesis of clopidogrel[J]. Chinese Journal of Medicinal Chemistry, 2007, 17(3): 163-165 |
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| Authors: | LIANG Mei-hao SHEN Zheng-rong |
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| Abstract: | Aim To improve the synthetic procedure of clopidogrel,a platelet aggregation inhibitor.Methods The target compound was synthesized from alpha-amino-(2-chlorophenyl)acetic acid via resolution,esterification,SN2 substitution,and cyclization.A new racemizaton and resolution procedure was developed in the preparation of( )-alpha-amino-(2-chlorophenyl)acetic acid.Results and conclusion The overall yield is 26.9%.The improved synthetic procedure has the advantage of low cost and is suitable for industrial production. |
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