Highly efficient one-pot,three-component synthesis of1,5-benzodiazepine derivatives  

作　　者：Xiao-Qing Li Lan-Zhi Wang 

机构地区：[1]The College of Chemistry and Material Science,Hebei Normal University

出　　处：《Chinese Chemical Letters》2014年第2期327-332,共6页中国化学快报（英文版）

基　　金：financial support from the National Natural Science Foundation of China(No.21276064);the Natural Science Foundation of Hebei Education Department(No.2008320);the Science Foundation of Hebei Normal University(No.2011Y04)

摘　　要：A general, mild and efficient protocol for the synthesis of ethyl 4-methyl-2-（thiophen）-2,5-dihydro-1,5- benzodiazepine-3-carboxylate is achieved for first time using H3PMo12O40 in ethanol at 0 ℃ by a one- pot, three-component condensation of various thiophene aldehydes, substituted o-phenylenediamines and ethyl acetoacetate. Compared with the conventional synthesis method, this procedure has the advantages of convenient operation, excellent yields, and environmentally benign. A plausible formation mechanism has been proposed. The structure of the products is characterized by1H NMR, IR, MS and elemental analysis.A general, mild and efficient protocol for the synthesis of ethyl 4-methyl-2-（thiophen）-2,5-dihydro-1,5- benzodiazepine-3-carboxylate is achieved for first time using H3PMo12O40 in ethanol at 0 ℃ by a one- pot, three-component condensation of various thiophene aldehydes, substituted o-phenylenediamines and ethyl acetoacetate. Compared with the conventional synthesis method, this procedure has the advantages of convenient operation, excellent yields, and environmentally benign. A plausible formation mechanism has been proposed. The structure of the products is characterized by1H NMR, IR, MS and elemental analysis.

关 键 词：ONE-POT Synthesis 1 5-Benzodiazepine derivative 

分 类 号：TQ463[化学工程—制药化工]