An efficient [2+2+2] benzannulation of phthalic acids/anhydrides with two alkynes was developed for synthesis of multisubstituted 1-naphthoic acids via Ru-catalyzed C-H activation. The reaction preceded well using atmospheric oxygen as the sole oxidant with high atom/step economies. Facilitated by the free carboxyl group, the products can be easily converted to diverse polycyclic molecules.

This study developed an efficient method for synthesis of multisubstituted 1-naphthoic acids using Ru-catalyzed C-H activation and double alkyne annulation under air, enabling easy conversion to diverse polycyclic molecules.

Paper

Synthesis of Multisubstituted 1-Naphthoic Acids via Ru-Catalyzed C-H Activation and Double Alkyne Annulation Under Air.

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