摘要
以文拉法辛为原料,分别以新的脱甲基试剂半胱氨酸钠盐和青霉胺钠盐制备了O-去甲基文拉法辛,收率为86%和82%。一锅中分别完成了半胱氨酸钠盐、青霉胺钠盐的制备与文拉法辛脱甲基反应,简化了操作步骤。最优反应条件为溶剂N-甲基吡咯烷酮,反应温度175℃,产物析晶pH值9.5。
The O-desmethylvenlafaxines were prepared from venlafaxine reacted with new demethylation reagents cysteine sodium and sodium penicillamine, respectively. The corresponding yields are 86% and 82%, respectively. Since the synthesis could be fulfilled in a one-pot approach by mixing cysteine sodium salt, sodium penicillamine preparation and venlafaxine demethylation together, the reaction was fairly simplified. The optimal reaction conditions are： N-methyl pyrrolidone as the solvent, reaction temperature of 175℃ and the pH value of 9.5 for product to crystallize.
出处
《应用化学》
CAS
CSCD
北大核心
2013年第5期608-610,共3页
Chinese Journal of Applied Chemistry
基金
河北省科技支撑项目(07215603D)
