Rh(iii)-catalyzed [4 + 1] cyclization of aryl substituted pyrazoles with cyclopropanols via C–H activation?

Organic & Biomolecular Chemistry Pub Date: 2022-12-19 DOI: 10.1039/D2OB02001G

Abstract

A rhodium-catalyzed formal [4 + 1]-cyclization reaction of aryl substituted pyrazoles with cyclopropanols via C–H bond activation/cyclization processes to selectively construct a series of carbonyl functionalized pyrazolo[5,1-a]isoindoles is described. The reaction features good functional group compatibility and a broad substrate scope with respect to both cyclization components with up to 84% yields. Mechanistic studies indicated that the C–H cleavage might be the rate-determining step in this transformation.

Graphical abstract: Rh(iii)-catalyzed [4 + 1] cyclization of aryl substituted pyrazoles with cyclopropanols via C–H activation
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