维拉佐酮的合成

摘要

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.