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

Author:

Shen Jian12,Cui Bo12,Huang Junwei12,Lin Shenghui2,Cui Xiuling12ORCID

Affiliation:

1. Engineering Research Centre of Molecular Medicine of Ministry of Education Key Laboratory of Fujian Molecular Medicine Key Laboratory of Precision Medicine and Molecular Diagnosis of Fujian Universities Key Laboratory of Xiamen Marine and Gene Drugs, School of Biomedical Sciences Huaqiao University Xiamen 361021 P. R. China

2. School of Biomedical Sciences Huaqiao University Quanzhou 362021 P. R. China

Abstract

AbstractA 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 RuII‐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.

Funder

Higher Education Discipline Innovation Project

Publisher

Wiley

Subject

Organic Chemistry,Physical and Theoretical Chemistry

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