维拉佐酮的合成工艺研究

The organic process research of vilazodone

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%.