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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 is carried out between ethyl 5-bromobenzofuran-2-carboxylate and 4-tert-butoxycarbonylpiperazine. If the catalyst is Pd (OAc) 2 / BINAP and the base is Cs2CO3, the product is mainly 5 (4-tert-butoxycarbonylpiperazinyl) benzofuran-2-carboxylate with 70% conversion rate; if the catalyst is Pd (dba) 2 / P Potassium alkoxide, the product has almost no ethyl 5- (4-tert-butoxycarbonylpiperazinyl) benzofuran-2-carboxylate.In this paper, the factors affecting the Buchwald-Hartwig coupling reaction are discussed.