Abstract
AbstractA concise synthesis of pyrazolo[1,5‐a]indole derivatives by copper‐catalyzed aerobic oxygenation and cyclization of indoles with oxime acetates is described. This protocol represents an elegant example of N‐1, C‐2, and C‐3 tri‐functionalization of indoles in one‐pot. Mechanistic studies indicate the reaction proceeds through a radical procedure. Oximes as an internal oxidant have been demonstrated to be a driver to initiate aerobic oxidation, which provides a new oxidative pattern for C‐H functionalization even with high atom‐ and step‐economy.
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