Preparation of chiral 1,4-benzodiazepin-2-one-derivatives by reaction of (s)-{60 -amino acid chloride hydrochlorides etc.

摘要

A process is disclosed for preparing optically active 1,4-diazepine-2-ones by reacting an acid chloride-hydrochloride of an optically active alpha -amino acid with a substituted o-amino benzophenone, to form an intermediate product and subsequently cyclizing the intermediate product to form the desired 1,4-diazepine-2-one. The process is carried out in inert organic or aqueous-organic solvents. The process eliminates the need for using alpha -amino acids having bound to the amino group a protective group which must be removed before cyclization.