摘要
通过对多条文拉法新盐酸盐合成路线的分析最终确定了通过缩合、加氢还原、甲基化的三步反应以对甲氧基苯乙腈为起始原料的合成方法。首先是缩合反应以对甲氧基苯乙腈和环己酮以及四丁基溴化氨为相转移催化剂合成α-(1-羟基环己基)-对甲氧基苯乙腈;第二步是以NiCl2/NaBH4作为还原剂,催化加氢合成1-[2-氨基-1-(4-甲氧基苯基)乙基]环己醇;最后一步以甲醛作为甲基化试剂进行甲基化反应合成盐酸盐文拉法新。其中相转移催化剂的使用,提高了反应收率,缩短了反应时间。
In this paper, we analyzed the process of synthesizing Venlafaxine hydrochloric acid and determined the three steps of contracting, hydrogenation deoxidation and methylating with methoxy phenylacetonitrile as starting material. First, the condensation of arylacetonitriles with cyclic ketones using aqueous NaOH under phase transfer catalysis gave almost quantitative yields of α- （1 - hydroxyl -cyclohexyl ） -4 -methoxybenzyl cyanide; second ,1 - [ 2 -Amino -1 - （4 -methoxy -phenyl - ）ethyl ] cyclohexanol which was synthesized by NiCl2/NaBH4 as reducer; and third, the methylation with formic acid and formaladehyde solution to give venlafaxine hydrochloride, among which the applied phase transfer catalysis can truncated the time and raise the yield of reaction.
出处
《淮阴工学院学报》
CAS
2007年第1期49-51,共3页
Journal of Huaiyin Institute of Technology
关键词
抗抑郁药
文拉法新
相转移催化剂
合成
antidepressant
Venlafaxine
phase transfer catalysis
synthesis
