摘要
目的:改进盐酸文拉法辛的合成工艺。方法:以对甲氧基苯乙腈和环己酮为原料,经缩合得α-(1-羟基环己基)-对甲氧基苯乙腈,再经还原,最后甲基化制备盐酸文法拉辛。以甲醇钠代替氢化钾作为缩合剂,以盐酸乙醇代替氯化氢气体,以甲苯代替乙醚,对此工艺进行了改进。结果:得到较好的工艺条件,总收率达到47.4%。结论:改进后的工艺降低了生产成本,易于工业化生产。
Objective： To improve the synthetic procedure of venlafaxine hydroehloride. Methods： α-（ 1- Hydroxyeyelohexyl）-p-methoxybenzyl cyanide was synthesized via condensation by using p-methoxybenzyl cyanide and eyelohexanone, then reduction, and methylation to give venlafaxine hydroehloride. Replacement of potassium hydride by sodium methoxide, replacement of hydrogen chloride by HCl-ethanol, and replacement of ether by toluene were in the improved procedure. Results： The suitable conditions were obtained, and the overall yield was 47.4%. Conclusion：The improved synthetic procedure is practical and easy to popularize in industry, and the production cost is reduced.
出处
《药学进展》
CAS
2006年第6期278-279,共2页
Progress in Pharmaceutical Sciences
关键词
盐酸文拉法辛
合成
工艺改进
Venlafaxine hydroehloride
Synthesis
Improved synthetic procedure
作者简介
通讯作者：王德传，副教授；研究方向：新药研究与开发；Tel：025-85391172；E-mail：wdc_dd1995@yahoo．com．cn
