Abstract
The first synthesis of diversely substituted isoxazole linked imidazo[1,2-a]azine derivatives via application of the Groebke-Blackburn-Bienayme (GBB) reaction with excellent yields is reported. This protocol proceeds via Cu(OTf)2-catalysed cascade three component reaction of isoxazole C-3(5) carbaldehydes and 2-aminopyridines/2-aminopyrimidines/2-aminopyrazines in the presence of isonitriles by forming one C–C, and three C–N bonds in a single-operation. The synthetic utility of this transformation is also extended through a gram scale synthesis. The salient features like clean reactions, short reaction time, good to excellent yields, high atom economy and easy purification procedures enacted this protocol as a practical contribution to the synthesis of medicinally valuable heterocycles.
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