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Preparation of chiral 1,4-benzodiazepin-2-one-derivatives by reaction of (s)--amino acid chloride hydrochlorides etc.
Preparation of chiral 1,4-benzodiazepin-2-one-derivatives by reaction of (s)--amino acid chloride hydrochlorides etc.
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机译:通过(s)-氨基酸氯化物盐酸盐等的反应制备手性1,4-苯并二氮杂-2-酮衍生物
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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 -amino acids having bound to the amino group a protective group which must be removed before cyclization.
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