扎利罗登合成工艺的改进

Improvement of synthesis process for Xaliproden hydrochloride

目的改进扎利罗登的合成工艺。方法以1-苄基-4-哌啶酮及1-溴-3-三氟甲苯为原料,经还原、消除、加成、成盐等反应合成扎利罗登。结果产品总收率为28.5%,并用质谱、氢谱等鉴定了目标物的结构。HPLC法检测纯度达到99.2%。结论改进后的方法优化了反应条件和投料比,缩短了反应时间,简化了操作步骤,适合工业化生产。

OBJECTIVE To improve synthetic route of Xaliproden hydrochloride.METHODS The product was synthesized from 1-benzyl-4-piperidone,1-bromo-3-trifluoromethyl benzene via several steps involving Grignard,reduction,elimination,addition and saltify reaction.RESULTS The total yield of Xaliproden was 28.5% .Xaliproden was examined by HPLC and the pure degree was over 99.2% .CONCLUSION The improved synthetic route optimized the synthetic process and have a further pilot manufacture.