Abstract

A series of 17 cyanoacetamides was synthesized for pharmacologic evaluation. Several synthetic methods were studied: C-alkylation, acylation of amines by ester, and acylation of amines by amides. The C-alkylation of cyanoacetamides was investigated in several solvent systems using various bases, and the results are reported. This method was adopted for the alkylation of the cyanoacetamides in a pressure-reaction vessel and utilized formamide and/or dimethylsulfoxide as solvent with potassium hydroxide as the basic reagent. Several of the compounds were obtained by the pyrolytic acylation of amine by amide. A series of 17 cyanoacetamides was synthesized for pharmacologic evaluation. Several synthetic methods were studied: C-alkylation, acylation of amines by ester, and acylation of amines by amides. The C-alkylation of cyanoacetamides was investigated in several solvent systems using various bases, and the results are reported. This method was adopted for the alkylation of the cyanoacetamides in a pressure-reaction vessel and utilized formamide and/or dimethylsulfoxide as solvent with potassium hydroxide as the basic reagent. Several of the compounds were obtained by the pyrolytic acylation of amine by amide.

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