a novel strategy of ugi-4cr/huisgen 1,3-dipolar synthesis of 1h-1,2,3-triazole-modified peptidoimetics

In this protocol, we report a novel approach for the synthesis of a new class of heterocyclic 1h-1,2,3-triazole-modified peptidoimetic compounds. the process consists of an ugi four-component condensation reaction of amines, an isocyanide, an aldehyde and acids followed by a huisgen 1,3-dipolar cycloaddition reaction with an azide group in the presence of a catalytic amount of cuso4.5h2o/sodium ascorbate. the copper-catalyzed huisgen cycloaddition reactions provide such a general synthetic method, with the resulting 1,2,3-triazoles being good peptide bond mimics. this protocol was highly efficient for structurally diverse heterocyclic molecules containing an active aldehyde group and will find applications in combinatorial chemistry, diversity-oriented synthesis, and drug discovery.