Demonstrates effective synthesis of diverse N2-substituted azaindazoles, suggesting practical applications in drug development.
N2-Substituted (aza)indazoles are versatile heterocycles that commonly feature in bioactive, drug-like molecules. We report a practical one-pot method developed as part of medicinal chemistry efforts to access these from amino (aza)benzaldehydes and a wide array of amines. The key oxidative N–N bond cyclization is mediated by PhI(OAc) 2, enabling rapid access to a breadth of N2 -functionalized (aza)indazoles. This protocol can also be scaled up in batch for multigram, chromatography-free synthesis.
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Fan et al. (2026) studied this question.
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