General Multicomponent Strategy for the Synthesis of 2-Amino-1,4-diazaheterocycles: Scope, Limitations, and Utility

Multicomponent reactions of primary 1,2‐ and 1,3‐diamines with carbonyl compounds and isocyanides resulting in the formation of diverse 2‐amino‐1,4‐diazaheterocycles are described. Lewis acids (LAs) promote the reactions effectively, and chlorotrimethylsilane (TMSCl) has been found to be a promoter of choice. The scope and limitations of the reactions with regard to each of the components are evaluated and discussed. Post‐IMCR modifications of the synthesized heterocycles have been elaborated. Novel multicomponent reactions based on primary 1,2‐ and 1,3‐diamines, carbonyl compounds, and isocyanides have beendeveloped as a general strategy for the synthesis of unique amino derivatives ofvarious privileged azaheterocycle structures, including pyrazines, 1,4‐diazepines, quinoxalines, and their fused andspirocyclic analogues.