An approach for the synthesis of 2-aryl-3-sulfonyl substituted quinolines through an electrochemical cascade annulation pathway

An electrochemical protocol for the synthesis of 2,3-disubstituted quinolines by reacting benzoxazinones with arylsulfonyl hydrazides was established under simple and mild conditions (room temperature and an undivided cell). The methodology does not require noble catalysts or external oxidants, providing a green and mild pathway for de novo synthesis of functional quinolines with excellent regioselectivity. Moreover, the method tolerated a variety of functional groups. Notably, the scaled-up experiment and follow-up procedures demonstrate the practicality of electrochemical synthesis.

Automated summary

An electrochemical protocol was developed for the synthesis of 2,3-disubstituted quinolines. The method is simple, mild, and does not require noble catalysts or external oxidants. It shows excellent regioselectivity and can tolerate various functional groups. The scaled-up experiment and follow-up procedures demonstrated the practicality of electrochemical synthesis.