Diketeneの利用研究(第3報) : Amine類のα-Acetamidoacyl化について

概要

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By the utilization of the marked reactivity of amines and diketene, α-acetamidoacyl derivatives of biologically active amines were synthesized in an attempt to decrease the toxicity of such amines. In this reaction (Chart 1), acetacetylated amines are submitted to the Schmidt reaction, and the compounds obtained are listed in Table I and II. It is desirable, in this reaction, to add sodium azide to the chloroform solution of the acetacylamide derivatives and then add conc. sulfuric acid dropwise, rather than its reverse of adding conc. sulfuric acid to the chloroform solution and then sodium azide. Otherwise, the Knorr reaction often occurs.
公益社団法人日本薬学会の論文
1970-12-25