Abstract
AbstractAn efficient and regioselective cyclization for construction of pyrazolo[3,4‐b]pyridines and methylene‐bridged bis(pyrazolo[1,5‐a]pyrimidines) has been established. It involves a [3+2+1] annulation of 3(5)‐aminopyrazole, N,N‐dimethylethanolamine (DMEA), with 1,2‐insertion of aryl methyl ketones or 2,1‐insertion of aryl alkynes. DMEA is oxidized through C(sp3)‐H activation to provide a single or triple carbon source.
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