维拉佐酮的合成

Synthesis of Vilazodone

以5-硝基苯并呋喃-2-羧酸乙酯为原料,经氢化得到5-氨基苯并呋喃-2-羧酸乙酯,与N,N-双(2-氯乙基)氨基甲酸叔丁酯发生成环反应得5-(4-叔丁氧羰基-1-哌嗪基)苯并呋喃-2-羧酸乙酯,再与甲酰胺反应制得5-(4-叔丁氧羰基-1-哌嗪基)苯并呋喃-2-甲酰胺,经盐酸甲醇溶液处理得重要中间体5-(1-哌嗪基)苯并呋喃-2-甲酰胺盐酸盐,最后与3-(4-氯丁基)-5-氰基吲哚缩合得到维拉佐酮。

Using 5- nitrobenzene and furan- 2- carboxylic acid ethyl ester as a raw material,after hydride reaction,amino coumarone- 2- 5- carboxylic acid ethyl ester was produced,with N,N- double（ 2- ethyl chloride）carbamate tert- butyl ester cyclization reaction,5-（ 4- tert- butyl carbonyl oxygen- 1- piperazine） coumarone- 2-carboxylic acid ethyl ester was produced,reacted with formamide,5-（ 4- tert- butyl carbonyl oxygen- 1- piperazine）coumarone- 2- formamide was produced dealled with hydrochloric acid methanol solution the important intermediate,5-（ 1- piperazine） coumarone- 2- formamide hydrochloride was produced,finally with 3-（ 4- chlorobutyl）- 5- cyano indole devery,Vilazodone was prepared.