Synthesis of Fused Imidazoles and Pyrimidinones from 2‐Aminoazines

Abstract Fused imidazole and pyrimidine heterocycles represent two important classes of organic compounds. Numerous synthetic methods have been developed for the synthesis of these compounds due to their diverse biological activities and potential pharmaceutical applications. This review provides a comprehensive assessment of the cutting‐edge methods used in the synthesis of fused heterocycles from pyridin‐2‐amines and their aza derivatives involving reaction with 1,3‐dicarbonyl compounds or α ‐halo carbonyl compounds. In addition, the Groebke‐Blackburn‐Bienaymé (GBB) reaction, metal‐mediated reactions and other related reaction systems have been considered. We summarize the pertinent literature on related synthetic methods in the period 2020 to 2023. The analysis provided can inform future developments directed at new cost‐effective approaches to the synthesis of fused imidazole and fused pyrimidine analogues.