盐酸舍曲林的合成工艺改进

Improved synthesis of sertraline hydrochloride

目的:改进盐酸舍曲林的合成工艺。方法:以α-萘酚为起始原料,经烷基化,甲胺胺化,Pd/C催化氢化,D-(-)扁桃酸拆分,成盐而合成盐酸舍曲林。结果:以α-萘酚计,总收率由文献的16.2%提高到31.5%;盐酸舍曲林的结构经红外、差热分析、核磁、质谱确证。结论:该方法工艺简单,适合工业化生产。

Objective： To improve synthesis of sertraline hydrochloride.Methods： Sertraline hydrochloride was synthesized from orthodichlorobenzene and α-naphthol by alkylation reaction,amination with methylimine,hydrogenation with Pd/C,resolution with D-（-）mandelic acid and salt formation.Results： The overall yield was raised from 16.2% to 31.5%.The structure of sertraline hydrochloride was verified by IR,DSC,1H-NMR and MS.Conclusion： The process is simple and suitable for the needs of industrial production.