甲磺酸多拉司琼的合成  

Synthesis of Dolasetron Mesilate

作　　者：郭跃龙[1] 胡振[2] 易超[2] 唐尧[2] 

机构地区：[1]江苏省省级机关医院,江苏南京210024 [2]江苏奥赛康药业股份有限公司,江苏南京211112

出　　处：《中国医药工业杂志》2012年第8期651-653,共3页Chinese Journal of Pharmaceuticals

摘　　要：3-环戊烯-1-甲酸甲酯(2)依次经间氯过氧苯甲酸和高碘酸氧化后,经Robinson-Schoepf反应制得3-甲氧羰基-7-氧代-9-氮杂二环[3.3.1]壬烷-9-乙酸甲酯(4),再经还原、羟基保护和成环反应制得(2,6,8,9a)-六氢-8-羟基-2,6-亚甲基-2H-喹啉-3(4H)-酮(7),最后与吲哚-3-羧酸反应后与甲磺酸成盐,制得5-HT3受体拮抗剂甲磺酸多拉司琼,总收率约12%(以2计)。Dolasetron mesilate, the 5-HT3 receptor antagomst, was enecarboxylate （2） by successively oxidation with m-CPBA and H104, and Robinson-Schoepf reaction to give methyl 3_methoxycarbonyl-7-oxo-9-azabicyclo[3.3.11 nonane-9-acetate （4）, which was subjected to reduction, protection, cyclization, reaction with indole-3-carboxylic acid and then salt formation with an overall yield of about 12%.

关 键 词：甲磺酸多拉司琼 5-HT3 受体拮抗剂 合成 

分 类 号：R975.4[医药卫生—药品]