One-Pot Construction of 3-Phthalimido-1,5-benzodiazepine-2-one Derivatives via in situ Activation of N,N-Phthaloyl-serine

Author:

Obara Nobuhiro1,Watanabe Takeshi2,Asakawa Tomohiro23,Kan Toshiyuki2,Tanaka Takao1

Affiliation:

1. Zeria Pharmaceutical Co., Ltd

2. School of Pharmaceutical Sciences, University of Shizuoka

3. Tokai University Institute of Innovative Science and Technology

Abstract

The Michael addition of dehydroalanine-activated ester in situ generated from N,N-phthaloyl-serine with o-phenylenediamine followed by cyclization has been established under mild conditions, which afforded 3-phthalimido-1,5-benzodiazepine-2-one derivatives in moderate to good yields.

Publisher

Georg Thieme Verlag KG

Subject

Organic Chemistry

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