文拉法新的合成工艺改进

An improved novel method of venlafaxine synthesis

目的 :为使文拉法新适于工业化生产 ,对其合成工艺作了适当改进。方法 :以对甲氧基苯乙酸为原料 ,经SOCl2 酰氯化 ,N,N—二甲基胺酰胺化 ,然后经 Ivanov反应和 KBH4/BF3 .Et2 O还原 ,最后和异丙醇 - HCl成盐制得文拉法新。结果 :成功制得目标化合物 ,总收率为 5 0 .3%。结论 :该方法操作简单、原料易得、收率高。

Objective: To synthesize venlafaxine with an improved novel method. Methods: p-methoxypheny-lethyl acid was reacted with SOCl_2 to produce acyl chloride,which was reacted with N,N-dimethylamine solution to get amide; then through Ivanov reaction and reduction by KBH_4/BF_3.Et_2O to yield venlafaxine. Results: Venlafaxine was successfully synthesized by using this method with an yield rate of 50.3%. Conclusion: The improved method is suitable for industrial production of venlafaxine.