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 ^,

1.
The College of Chemistry and Material Science, Hebei Normal University, Shijiazhuang 050024, China

Corresponding author: Lan-Zhi Wang,
Received Date: 17 July 2013
Available Online: 6 November 2013
Fund Project: 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)

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.
- One-pot,
- Synthesis,
- 1,5-Benzodiazepine derivative
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