Site-Selective C8-Alkylation of Quinoline N-Oxides with Maleimides under Rh(III) Catalysis

The site-selective modification of quinolines and their analogs has emerged as a pivotal topic in medicinal chemistry and drug discovery. Herein, we describe the rhodium(III)catalyzed C8-alkylation of quinoline N-oxides with maleimides as alkylating agents, resulting in the formation of bioactive succinimide-containing quinoline derivatives. The reaction proceeds under mild conditions with complete functional group tolerance.

Automated summary

The site-selective modification of quinolines and their analogs using rhodium(III) catalysis has led to the synthesis of bioactive succinimide-containing quinoline derivatives with high tolerance to functional groups.