Tetrahedron

Synthesis of 5-arylpyrrolo [2, 1-c][1, 4] benzodiazepines under mild cyclodehydration conditions

L Legerén, D Domínguez

Index: Legeren, Loreto; Dominguez, Domingo Tetrahedron, 2010 , vol. 66, # 14 p. 2718 - 2722

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Citation Number: 2

Abstract

The efficiency of a cyclodehydration reaction leading to benzodiazepinones is markedly improved by N-methylation of the amide link connecting the nucleophile and the electrophile, which is attributed to its favouring both the more reactive E-rotamer and the exit of the leaving group.