We disclose a new platform for C(sp3)-directed C–H annulations to generate valuable heterocycles from readily available starting materials. A commercially available one carbon linchpin is leveraged to access alkyl boron species from simple anilines. Rhodium-catalyzed C(sp3) transmetallation from this key intermediate provides a C–Rh bond appropriately positioned for ortho-C–H activation, enabling formation of C,C-rhodacycles. With the addition of a variety of alkyne coupling partners, diverse dihydroquinolines are synthesized.
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Hollerbach et al. (2024) studied this question.
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