[一种改进的文拉法辛合成新方法]
[An improved novel method of venlafaxine synthesis].
作者信息
Sheng Rong, Liu Tao, Hu Yong-zhou
机构信息
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, China.
出版信息
Zhejiang Da Xue Xue Bao Yi Xue Ban. 2004 Jan;33(1):77-9. doi: 10.3785/j.issn.1008-9292.2004.01.018.
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(2)O to yield venlafaxine.
RESULT
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.
目的
用一种改进的新方法合成文拉法辛。
方法
对甲氧基苯乙酸与亚硫酰氯反应生成酰氯，酰氯再与N,N -二甲基胺溶液反应得到酰胺；然后经过伊万诺夫反应，并用硼氢化钾/三氟化硼乙醚络合物还原，得到文拉法辛。
结果
用该方法成功合成了文拉法辛，产率为50.3%。
结论
该改进方法适用于文拉法辛的工业化生产。
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