盐酸利莫那班的合成工艺研究  

Synthesis of rimonabant

作　　者：王玮[1] 陈国广[1] 方正[1] 唐海涛[1] 韦萍[1] 

机构地区：[1]南京工业大学制药与生命科学学院,材料化学工程国家重点实验室,南京210009

出　　处：《中国新药杂志》2009年第12期1152-1154,共3页Chinese Journal of New Drugs

摘　　要：目的:确定并优化减肥药盐酸利莫那班的合成工艺。方法:对氯苯丙酮经硅烷化成烯醇硅醚,与草酸单酰氯单乙酯缩合得α,γ-二酮酸酯,成腙、环合、水解、酰胺化并成盐得盐酸利莫那班。结果:目标产物化学结构经MS,1HNMR及元素分析确证,总产率达34.2%。结论:本方法反应条件温和,操作简便,产率较高,适用于工业化生产。Objective： To optimize the synthetic route of rimonabant. Methods： Rimonabant hydrochloride was synthesized from 4-chloropropiophenone as starting material by silylation, aeylation with ethyl oxalyl chloride to give α,γ-diketo ester, which was subjected to hydrazone reaction, cyclization, hydrolysis, amidation and salt formation. Results： The structure of the target compound was confirmed by MS, 1^HNMR, element analysis, and the overall yield was up to 34.2%. Conclusion ： This synthetic route is of mild reacting condition, easy operation and relative high yield and is worthy to be pilot.

关 键 词：利莫那班 减肥药 合成 

分 类 号：R977[医药卫生—药品]