文献类型：期刊文献

中文题名：5-(4-叔丁氧基羰基哌嗪基)苯并呋喃-2-甲酸乙酯的合成

英文题名：Synthesis of Ethyl 5-(4-tert-Butyloxycarbonyl-1-piperazinyl)benzofuran-2-carboxylate

作者：封静[1];王成云[1];周长凯[1];左虎进[1];沈永嘉[1]

机构：[1]华东理工大学结构可控先进功能材料及其制备教育部重点实验室精细化工研究所,上海200237

年份：2011

卷号：31

期号：2

起止页码：203

中文期刊名：有机化学

外文期刊名：Chinese Journal of Organic Chemistry

收录：CSTPCD;;Scopus;北大核心:【北大核心2008】；CSCD:【CSCD2011_2012】；

语种：中文

中文关键词：哌嗪;苯并呋喃;甲酸乙酯;合成;Buchwald-Hartwig偶联

外文关键词：piperazine; benzofuran; ethyl formate; synthesis; Buchwald-Hartwig coupling reaction

摘要：5-溴苯并呋喃-2-甲酸乙酯与4-叔丁氧基羰基哌嗪进行Buchwald-Hartwig偶联反应,若催化剂是Pd(OAc)2/BINAP,碱是Cs2CO3,则产物主要是5-(4-叔丁氧基羰基哌嗪基)苯并呋喃-2-甲酸乙酯,转化率达70%;若催化剂是Pd(dba)2/P(t-Bu)3,碱是叔丁醇钾,则产物中几乎没有5-(4-叔丁氧基羰基哌嗪基)苯并呋喃-2-甲酸乙酯.文中讨论了影响这个Buchwald-Hartwig偶联反应的因素.
Buchwald-Hartwig coupling reaction between ethyl 5-bromobenzofuran-2-carboxylate and tert-butyl piperazine-1-carboxylate was studied.When Pd（OAc）2/BINAP was employed as catalyst and Cs2CO3 as base,the major reaction product was ethyl 5-（4-tert-butyloxycarbonyl-1-piperazinyl）benzofuran-2-carboxylate,with a reaction conversion rate of 70%.While Pd（dba）2/P（t-Bu）3 was employed as catalyst and potassium tert-butoxide as base,nearly no ethyl 5-（4-tert-butyloxycarbonyl-1-piperazinyl）benzofuran-2-carboxylate was observed.Some factors of affecting the reaction were discussed as well.