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Highly efficient one-pot,three-component synthesis of 1, 5-benzodiazepine derivatives
Authors:Xiao-Qing Li  Lan-Zhi Wang
Institution:The College of Chemistry and Material Science, Hebei Normal University, Shijiazhuang 050024, China
Abstract: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 onepot, 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 by 1H NMR, IR, MS and elemental analysis.
Keywords:One-pot  Synthesis  1  5-Benzodiazepine derivative
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