R-莫达非尼的合成及条件优化  

Synthesis and craftsmanship optimization of R-modafinil

作　　者：卢来春[1] 卢华 王朝安[3] 胡小刚[1] 赵艳艳[1] 孟德胜[1] 

机构地区：[1]第三军医大学大坪医院药剂科,重庆400042 [2]山东即墨市中医院妇产科,山东即墨266000 [3]解放军报社门诊部,北京100832

出　　处：《第三军医大学学报》2009年第23期2361-2362,共2页Journal of Third Military Medical University

摘　　要：目的合成R-莫达非尼,并对合成条件进行优化。方法以二苯甲醇为原料,与2-巯基乙酸反应合成2-二苯甲基硫代乙酸,再经成酯保护、H202氧化、脱保护、拆分,最后氨化合成R-莫达非尼。结果合成了目标化合物,结构经旋光仪、13CNMR、1HNMR、IR分析确证,总收率为10.1%。结论合成思路和路线切实可行。Objective To synthesize R-modafinil and optimize the synthetic route. Methods Target molecule R-modafinil was synthesized from diphenylmethanol and mercapto-acetic acid by a six-step reaction,including condensation,esterification,oxidation,deprotection,split,and ammonification. Results The target molecule was synthesized and identified by spectropolarimeter,13C NMR,1H NMR,and IR. The total yield was 10.1%. Conclusion Our synthesis of R-modafinil is accomplished with a feasible synthetic route.

关 键 词：R-莫达非尼 合成 

分 类 号：R916.4[医药卫生—药学] R971.7