摘要
目的对2-卤代-2-(2-氟苯基)-1-环丙基乙酮中间体合成工艺进行改进。方法以邻氟苯乙酸为起始原料,经与异丙基溴化镁格式试剂反应后与环丙基甲酸甲酯反应得到2-(2-氟苯基)-1-环丙基乙酮,再经用二溴海因(DCDMH)或二氯海因(DBDMH)作为卤代试剂,在自由基引发剂及光照下高收率的得到普拉格雷关键中间体2-卤代-2-(2-氟苯基)-1-环丙基乙酮。结果产物含量93%以上,其结构经1H-NMR,MS和IR确证。结论该工艺合理、可行,为工业化生产提供了实验依据。
Objective To study the Synthesis of 2-halogeno-2-（2-fluorophenyl）-1-cyclopropy[ethanone. Methods A key intermediate of Prasugrel,was synthesized from 2-Fluorophenylacetic acid via Grignard reaction with Isopropylmagnesium bromide and Methyl cyclopro- pane carboxylate to give 2-fluorophenyl）-1-cyclopropylethanone, followed by halogenation with DBDMH or DCDMH by use of a radical initiator and light. Results The content of the product is more than 93%. Conclusion The process is reasonable and feasible, and pro- vides the basis for industrial production.
出处
《安徽医药》
CAS
2013年第11期1839-1841,共3页
Anhui Medical and Pharmaceutical Journal
基金
广东省科技计划项目(No 2010B031600136)
