A general and efficient route to 6‐methyl‐pyrazin‐2‐yl‐amines: Alkylation of 2,6‐dichloropyrazine <i>via</i> malonate derivatives

Abstract

Abstract magnified image We have developed a convenient two‐stage process for the synthesis of 6‐methylpyrazine‐2‐yl‐amines from commercially available materials. The procedure involves the synthesis of (6‐chloro‐pyrazin‐2‐yl)‐acetic acid via arylation of diethyl malonate and in situ hydrolysis/decarboxylation. A second decarboxylation takes place under the subsequent amination conditions allowing simple and efficient access to the intended pyrazines.