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Updated: Dec 22, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Gold(iii)-catalyzed azide-yne cyclization/O-H insertion cascade reaction for the expeditious construction of
Jingjing Huang1, Han Su2, Ming Bao1
1Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, Guangdong 510006, China. zhangyq65@mail.sysu.edu.cn xuxinfang@mail.sysu.edu.cn.
Abstract:
A gold-catalyzed 6-endo-dig azide-yne cyclization/O-H insertion cascade reaction of azide-tethered alkynes with alcohols has been developed, and it provides an expeditious access to 3-alkoxy-4-quinoline derivatives in good to high yields under mild and neutral reaction conditions with broad substrate generality. The utility of this method is emphasized by a scalable experiment and concise total synthesis of a bioactive natural product Leiokinine A, and other bioactive quinoline analogs.
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