氢溴酸沃替西汀合成工艺改进

摘要

The synthesis of vortioxetine was improved to raise yield and simplify the process. Vortioxe-tine hydrobromide was synthesized from 1-fluoro-2-nitrobenzene and 2,4-dimethylbenzenethiol by nucle-ophilic substitution, reduction, condensation and salifying to obtain the objective compound. Structures were confirmed by 1H-NMR and MS. In this route, the raw materials are cheap, the reactions are simple without any catalyzer and the yield is high. This route is suitable for industrial production. The total yield is 57.9% (based on 2,4-dimethylbenethiol).%改进氢溴酸沃替西汀的合成工艺，以提高收率，简化处理过程。以2，4-二甲基苯硫酚和邻氯硝基苯为起始原料，经亲核取代、还原、缩合、成盐制得目标化合物。目标化合物经过1H-NMR，MS得到确证。该路线原料易得，后处理简单，反应条件温和，无需任何催化剂、缚酸剂。以2，4-二甲基苯硫酚计，总收率为57.3%，适合工业化生产。