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Updated: Jan 7, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Solvent-Controlled [4 + 2] Annulation Reaction: Selective Synthesis of 1,4-Dihydroquinolines/Quinolines
Mao-Lin Liao1, Qin Guo1, Yu Ao1
1Key Laboratory of Carbohydrate Chemistry and Biotechnology, Ministry of Education, School of Life Science and Health Engineering, Jiangnan University, Wuxi 214122, P. R. China.
Abstract:
A practical strategy was developed for the selective synthesis of 1,4-dihydroquinolines or quinolines through [4 + 2] annulation of aminobenzyl phosphonium salts (ABPS) and enaminones. In the process, solvent control alone enables the highly selective progression of this reaction, omitting the need for any metal catalysts or basic additives, providing an array of 1,4-dihydroquinolines or quinolines by using THF or DMSO, respectively. The reaction was featured with mild reaction conditions, readily accessible reagents, excellent substrate generality, and high yields.
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