Three-Component Couplings among Heteroarenes, Difluorocyclopropenes, and Water via C–H Activation

Three-component couplings have been realized for efficiently constructing various nitrogen-containing skeletons via C–H activation, where difluorocyclopropenes have been first identified as coupling partners. Many substrates including sp² and sp³ C–H substrates were well tolerated, furnishing the corresponding products in good yields. Furthermore, a catalyst-dependent reaction was also developed, enabling divergent construction of two different frameworks. The application value of these reactions was demonstrated in gram-scale experiments with as little as 1 mol % catalyst.