One‐Pot, Multi‐Component Synthesis of Novel 2‐Amino‐[1,2,4]triazolo[1,5‐ a ]pyrimidine‐6‐carboxamide Derivatives as Antiproliferative Agents

A novel series of 2‐amino‐[1,2,4]triazolo[1,5‐ a ]pyrimidine‐6‐carboxamide derivatives has been achieved successfully via an efficient one‐pot three‐component Biginelli‐like heterocyclization reaction between different benzaldehydes, 1 H ‐1,2,4‐triazole‐3,5‐diamine, and N ‐substituted acetoacetamides in the presence of p ‐toluenesulfonic acid as a catalyst. Moreover, the effects of different conditions on the reaction were well investigated. In addition, cancer cell growth inhibition activity for these target compounds was also explored, and analogue 5 l demonstrated the most potent cytotoxic activity against different cancer cells. These finds indicat that 2‐amino‐[1,2,4]triazolo[1,5‐ a ]pyrimidine‐6‐carboxamide core could be well worth further optimization as a potential scaffold for development of anticancer agents.