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A new method for the synthesis of dihydroimidazo[1,2-a][1,3,5]triazin-4(6H)-ones via copper(I)-catalyzed hydroamination was developed. In addition, for the first time, iodoalkynes were shown to participate in the copper(I)-catalyzed intramolecular hydroamination reaction with exclusive formation of E-isomers.

Synthesis of 7-Aza-5-deazapurine Analogues via Copper(I)-Catalyzed Hydroamination of Alkynes and 1-Iodoalkynes