莫达非尼左旋异构体的合成工艺研究  

Synthesis of the levoisomer of modafinil

作　　者：王珊[1] 叶晓娟[1] 钱珊[1] 吴勇[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《中国药物化学杂志》2009年第2期106-108,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的合成新型中枢兴奋药物莫达非尼的左旋异构体。方法以二苯甲醇和巯基乙酸为起始原料,经缩合、酯化、氧化、水解,得到(±)-二苯甲基亚硫酰基乙酸,用(S)-(-)-α-甲基苄胺拆分得到(-)-二苯甲基亚硫酰基乙酸,再经酯化、氨解,得到目标化合物。结果目标化合物结构经核磁共振氢谱和质谱确证。结论该合成方法,原料廉价易得,实验操作简单。Aim To synthesize the levoisomer of modafinil. Methods Benzhydrol and thioglycolic acid was used as the starting material to synthesize racemic （diphenylmethanesulfinyl） acetic acid by condensation, esterification, oxidation, hydrolysis. （ - ） -（Diphenylmethanesulfinyl） acetic acid was obtained by resolution with （S）-（ - ）-ot-methylbenzylamine. Then the target compound was obtained by esterification , ammonolysis. Results The structure of target compound was confirmed by ^1H-NMP, MS. Conclusion The raw materials in this route are cheap, and the experimental section is easy to control.

关 键 词：(-)-莫达非尼 拆分 (S)-(-)-α-甲基苄胺 二苯甲醇 巯基乙酸 

分 类 号：R914[医药卫生—药物化学]