Synthesis of C3-sulfone substituted naphthols via rhodium(iii)-catalyzed annulation of sulfoxonium ylides with alkynylsulfones

C-H activation of sulfoxonium ylides catalyzed by rhodium(iii) with subsequent annulation by alkynylsulfones was accomplished. This methodology offers a step-economical approach for assembling C3-sulfone-substituted naphthols with a high level of regioselectivity that is complementary to previous protocols. The approach has an extensive substrate spectrum and broad functional group tolerance.

Automated summary

The C-H activation of sulfoxonium ylides catalyzed by rhodium(III) followed by annulation with alkynylsulfones allows for the high regioselective assembly of C3-sulfone-substituted naphthols. This method is a step-economical approach that is complementary to previous protocols, with a wide substrate scope and broad functional group tolerance.