维拉佐酮的合成工艺研究  

The organic process research of vilazodone

作　　者：田野[1] 童仲夏 梁振[1] 焦恩强 郭春[1] 

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《中国药物化学杂志》2015年第2期118-121,共4页Chinese Journal of Medicinal Chemistry

基　　金：国家基础科学人才培养基金项目(J1103606)

摘　　要：目的对维拉佐酮的合成工艺进行研究。方法以对硝基苯酚为起始原料,经甲酰化、环合、还原、N-烃化及氨解5步反应得到关键中间体5-(哌嗪-1-基)苯并呋喃-2-甲酰胺(8);以5-溴吲哚为起始原料,经氰化、酰基化、还原3步反应得到另一中间体3-(4-氯丁基)-1H-吲哚-5-甲腈(12);中间体8与12经烃化反应制得目标化合物维拉佐酮。结果与结论目标化合物的结构经1H-NM R、M S谱确证,总收率10.9%。The antidepressive drug vilazodone was synthesized from a convergent synthesis, using 2-hydroxy- 5-nitrobenzaldehyde as the starting material, the key intermediate 8,5- （ piperazin- 1 -yl ） benzofuran-2-carboxamide, was obtained via formylation, cyclization, reduction, N-alkylation, and ammonolysis reaction; using 5- bromo-1H-indole as the starting material,intermediate 12 was obtained via cyanation, Friedel-Crafts acylation and reduction. We got the final product after intermediate 8 reacted with 12 in the base conditions. The struc- ture of the target compound was confirmed by ^1H-NMR and MS,in a yield of 10. 9%.

关 键 词：维拉佐酮 抗抑郁药 工艺改进 

分 类 号：R914.5[医药卫生—药物化学]