ChemInform Abstract: Efficient Synthesis of Aminomethylated Azaindoles and Corresponding Pyrrole‐Fused Derivatives by Copper‐Catalyzed Domino Multicomponent Coupling and Cyclization.

Abstract Efficient methods for the synthesis of aminomethylated azaindole derivatives via domino copper-catalyzed multicomponent coupling and cyclization have been developed. Using various secondary amines and aldehydes, N -substituted 3-ethynyl-4-aminopyridine was converted to substituted azaindoles in moderate to excellent yields. By use of a 3,4-diaminopyridine derivative bearing two alkynyl groups, the corresponding pyrrole-fused azaindoles were synthesized by controlled stepwise cyclization.