Rh()-catalyzed aldehydic and aryl C-H alkylation with cyclopropanols 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. Herein, we developed an efficient C-H alkylation of 2-aminobenzaldehydes and anilines employing cyclopropanol as an alkylating agent under Rh( iii )-catalysis for accessing a wide range of 1,4-diketones and β-aryl ketones in good to excellent yields.