期刊论文

Peng, D.-M.

中文

中国新药杂志

1003-3734

2011

20

14

1344-1346

长沙市科技计划项目（k1009016-11） 高等学校博士学科点专项科研基金资助项目（20090162120013）

本校为第一且通讯机构

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...