Highly efficient one-pot, three-component synthesis of 1, 5-benzodiazepine derivatives

Citation: Xiao-Qing Li, Lan-Zhi Wang. Highly efficient one-pot, three-component synthesis of 1, 5-benzodiazepine derivatives[J]. Chinese Chemical Letters, 2014, 25(2): 327-332. shu

Highly efficient one-pot, three-component synthesis of 1, 5-benzodiazepine derivatives

Xiao-Qing Li ,
Lan-Zhi Wang ^,

通讯作者: Lan-Zhi Wang,

基金项目:
We are grateful for financial support from the National Natural Science Foundation of China (No. 21276064) (No. 21276064)

the Natural Science Foundation of Hebei Education Department (No. 2008320) (No. 2008320)

the Science Foundation of Hebei Normal University (No. 2011Y04). (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 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.

关键词:

English

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