Rh(III)-Catalyzed Direct C-H Cyclization of N-Nitrosoanilines with 1,3-Dicarbonyl Compounds: A Route to Tetrahydrocarbazol-4-ones

A novel and efficient Rh(III)-catalyzed direct C-Hbondtandem annulation of N-nitrosoanilines with 1,3-dicarbonylcompounds through two C-H bond cleavage was developed. Thisprotocol provides a rapid access to a series of valuable tetrahydrocarbazol-4-oneswith the feature of readily available starting materials, broad functionalgroup tolerance, and in situ generation of carbene precursors. Importantly,some reaction products exhibited promising antiproliferative activityin cancer cell lines.

Automated summary

This article reports a novel and efficient Rh(III)-catalyzed direct C-H bond tandem annulation, which involves the cleavage of two C-H bonds and leads to a series of valuable tetrahydrocarbazol-4-ones. The method offers several advantages, including readily available starting materials, broad functional group tolerance, and in situ generation of carbene precursors. Importantly, some reaction products showed promising antiproliferative activity in cancer cell lines.