氘标记盐酸苯环壬酯的合成  

Synthesis of Deuterated Phencynondte Hydrochloride

作　　者：史卫国[1] 陈家骏[1] 樊士勇[1] 何新华[1] 陈兰福[1] 龚雄麒[1] 仲伯华[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《同位素》2011年第B12期112-115,共4页Journal of Isotopes

基　　金：国家自然科学基金重大项目分题资助(作用于M受体手性分子的药理学研究203900508);"重大新药创制"国家科技重大专项资助(一类抗晕新药左旋盐酸苯环壬酯的临床研究009ZXJ09004-067)

摘　　要：为了开展盐酸苯环壬酯及其光学异构体药代动力学研究,确定代谢途径,进行代谢差异比较,对盐酸苯环壬酯进行了稳定同位素氘标记合成研究。以五氘溴苯为原料,先由格氏反应生成D代中间体α-环戊基-α-D5-苯基羟乙酸乙酯,再经三步反应得到定位标记的盐酸氘代苯环壬酯。该合成路线简捷,同位素原料易得,引入标记原子的步骤短,反应条件较易控制,氘丰度达99%,经质谱、核磁确证结构与盐酸苯环壬脂一致。The experimental details for the preparation of phencynondte labelled with five deuteriums with high chemical purity and isotopic enrichment were researched. Deuterated intermediate compound a-cyclopentyl-a-Ds-phenyl-glycolate was synthesized first by Grignard reaction from bromobenzene-d5, the final product deuterated phencynondte hydrochloride was then prepared through next three steps reaction with excellent chemical purity and isotopic enrichment. D abundance of synthetic deuterated phencynondte hydrochloride was 99 %, the compound was identified by MS and 1H-NMR.

关 键 词：氘标记 盐酸苯环壬酯 药物合成 

分 类 号：TQ241[化学工程—有机化工] TQ122