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Communication | Regular issue | Vol 48, No. 7, 1998, pp.1331-1335
Published online, 1st January, 1970
DOI: 10.3987/COM-98-8163
A Novel Synthesis of 1,3-Benzodiazepin-2-ones Using Intramolecular Heck Reaction

Masahito Hayashi, Hiroshi Sai, and Hiroshi Horikawa*

*Lead Optimization Research Laboratory, Tanabe Seiyaku Co.Ltd., 2-2-50, Kawagishi, Toddda, Saitama 335-8505, Japan


The formation of the skeleton of 1,3-benzodiazepin-2-one could be efficiently achieved by intramolecular Heck reaction. This methodology was well applicable to the preparation of optically pure 4-substituted 1,3-benzodiazepin-2-ones starting from easily available α-amino acids.