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■ A Practical Route to Quinolines from Anilines

Hidetoshi Tokuyama, Masashi Sato, Toshihiro Ueda, and Tohru Fukuyama*

*Graduate School of Pharmaceutical Sciences, University of Tokyo, CREST, The japan Science and Technology Corporation (JST), 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan

Abstract

A practical route to quinoline from anilines through acid-mediated cyclization of 3-(N-aryl-N-sulfonylamino)propionaldehydes has been developed. Treatment of the cyclization products, dihydroquinoline intermediates with KOH in DMSO leads to substituted quinolines.