Rh(III)-catalyzed aldehydic and aryl C-H alkylation with cyclopropanols via C-H/C-C bond activation.

Herein, we report Rh(III) catalyzed aldehydic or aryl C-H alkylation via C-C bond activation of cyclopropanols, facilitating the synthesis of β-functionalized ketones. The protocol employs cyclopropanol as the alkylating agent with 2-aminobenzaldehyde or aniline derivatives to access a variety of unsymmetrical 1,4-diketones or β-aryl ketones, respectively. The practicality of these transformations is showcased through the modification of natural products, gram-scale synthesis, broad substrate scope and postfunctionalizations.