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An efficient synthesis of dihydro-isoquinolines via a Pd-catalyzed double C-H bond [a C(sp 2 )-H and a C(sp 3 )-H bond] activation/annulation (CHAA) reaction is presented. This methodology features a short reaction time, high atom economy (loss of H 2 O only) and the formation of a sterically less favoured tertiary C-N bond. This fast (30 min) and environmentally benign radical C-H activation approach has demonstrated the potential direction for the future design/development of fast and efficient C-H direct functionalization processes.

Modular synthesis of dihydro-isoquinolines: palladium-catalyzed sequential C(sp2)–H and C(sp3)–H bond activation

Modular synthesis of dihydro-isoquinolines: palladium-catalyzed sequential C(sp²)–H and C(sp³)–H bond activation