Abstract

AbstractA completely regioselective, environmentally benign strategy for the facile synthesis of biologically important imidazole‐fused nitrogen‐bridgehead heterocycles has been developed using glycerol/water 4:1 as a green promoting media. The methodology involves the simple coupling of 2‐halocarbonyl compounds with 2‐aminopyridines, 2‐aminopyrimidines, 2‐aminopyrazines to obtain a variety of 2‐aryl substituted imidazo‐pyridines, imidazo‐pyrimidines and imidazo‐pyrazines containing bridgehead nitrogen. This protocol eliminates the use of toxic catalysts and volatile organic solvents ‐ two key principles in the development of a green chemical process. Other significant highlights include mild reaction conditions, operational simplicity, short reaction times, easy workup and purification process, high yields and potential for scale‐up.

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