One-Pot Synthesis of Benzodiazepines through RuII-Catalyzed Regioselective [5+2] Annulation of N-Aryl Amidines with Alkynyl Cyclobutyl Acetates

被引:3
|
作者
Shen, Jian [1 ,2 ]
Cui, Bo [1 ,2 ]
Huang, Junwei [1 ,2 ]
Lin, Shenghui [2 ]
Cui, Xiuling [1 ,2 ]
机构
[1] Huaqiao Univ, Engn Res Ctr Mol Med, Key Lab Precis Med & Mol Diag Fujian Univ, Sch Biomed Sci,Key Lab Fujian Mol Med,Key Lab Xiam, Xiamen 361021, Peoples R China
[2] Huaqiao Univ, Sch Biomed Sci, Quanzhou 362021, Peoples R China
关键词
5+2] Cyclization; Alkynyl cyclobutyl acetates; Benzodiazepines; N-Aryl amidines; Ruthenium catalysis; C-H ACTIVATION; RING-CLOSING METATHESIS; BOND ACTIVATION; RH(III)-CATALYZED SYNTHESIS; DIVERGENT COUPLINGS; IMIDAMIDES; STRATEGY; ACCESS; DERIVATIVES; CYCLIZATION;
D O I
10.1002/ejoc.202300064
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A highly efficient strategy to construct benzo[d][1,3]diazepines via selective C-H bond activation of N-aryl amidines and coupling with alkynyl cyclobutyl acetates was achieved successfully by Ru-II-catalyzed [5+2] cyclization. This protocol features excellent regioselectivity, wide substrate tolerance, mild reaction conditions, which might be potentially applied in the discovery of lead compounds for the developing new drugs.
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页数:4
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