A simple and efficient method for synthesis of 5,7‐disubstituted pyrazolo[1,5‐a]pyrimidines is reported. The synthetic route involved first a one‐pot two‐step synthesis of 7‐substituted pyrazolo[1,5‐a]pyrimidin‐5‐ones from the reaction of 3‐aminopyrazole 1 with activated alkynes. These compounds were used as key intermediates to access, with excellent yields, a library of new 5,7‐disubstituted pyrazolo[1,5‐a]pyrimidines, which are known for their wide range of biological activities, through C–O bond activation with PyBroP (bromotripyrrolidinophosphonium hexafluorophosphate) as an activator reagent.
A convenient and efficient synthetic route to C3-arylated 7-trifluoromethylpyrazolo[1,5-a]pyrimidin-5-one derivatives has been reported starting from 3-bromo-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-5-one through a Suzuki–Miyaura cross-coupling reaction.
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