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Updated: Jan 13, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Metal-free quinoline synthesis via Brønsted acid-promoted cyclization of ene-ynamides
Yijie Wang1, Yu Li1, Lisha Zhang1
1Pingyuan Laboratory, State Key Laboratory of Antiviral Drugs, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan 450001, P.R. China. changjunbiao@zzu.edu.cn.
Abstract:
We report a metal-free strategy for the efficient synthesis of polysubstituted quinolines via Brønsted acid-promoted cyclization of readily accessible ene-ynamides. Promoted by stoichiometric TfOH under mild conditions (30 °C), this method transforms simple, modular substrates into a wide range of quinoline derivatives in a single step, eliminating the need for precious-metal catalysts or prefunctionalized reagents. Its broad functional group tolerance and successful gram-scale operation underscore the method's practical utility and potential for broader application.
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