Efficient synthesis of aminomethylated azaindoles and corresponding pyrrole-fused derivatives by copper-catalyzed domino multicomponent coupling and cyclization
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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.
Tetrahedron 68(6), 1695-1703, 2012-02