莫达非尼左旋异构体的合成工艺研究

Synthesis of the levoisomer of modafinil

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.