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Facile synthesis of 1,2,4,5-tetrahydro-1,4-benzodiazepin-3-ones via cyclization of N-alkoxy α-halogenoacetamides with N-(2-chloromethyl)aryl amides

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Abstract

A facile and efficient cyclization of N-alkoxy α-halogenoacetamides with N-(2-chloromethyl)aryl amides has been achieved for rapid access to 1,2,4,5-tetrahydro-1,4-benzodiazepine-3-one derivatives (up to 95% yield). The intriguing features of this intermolecular cyclization include its mild reaction conditions and easy handling for scalable synthesis.

Graphical abstract: Facile synthesis of 1,2,4,5-tetrahydro-1,4-benzodiazepin-3-ones via cyclization of N-alkoxy α-halogenoacetamides with N-(2-chloromethyl)aryl amides

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Publication details

The article was received on 18 Oct 2019, accepted on 01 Nov 2019 and first published on 01 Nov 2019


Article type: Communication
DOI: 10.1039/C9OB02260K
Org. Biomol. Chem., 2019, Advance Article

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    Facile synthesis of 1,2,4,5-tetrahydro-1,4-benzodiazepin-3-ones via cyclization of N-alkoxy α-halogenoacetamides with N-(2-chloromethyl)aryl amides

    Q. Jin, D. Zhang and J. Zhang, Org. Biomol. Chem., 2019, Advance Article , DOI: 10.1039/C9OB02260K

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