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Updated: Mar 7, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Palladium-catalyzed domino Heck/intermolecular cross-coupling: efficient synthesis of 4-alkylated isoquinoline
Tuanli Yao1, Tao Liu1, Changhui Zhang1
1College of Chemistry and Chemical Engineering, Shaanxi University of Science and Technology, 6 Xuefu Road, Weiyang District, Xi'an, Shaanxi 710021, China. yaotuanli@sust.edu.cn.
Abstract:
A highly efficient Pd-catalyzed Heck-type cascade process with 2-(1-alkynyl)benzaldimines has been developed, which provides access to a broad range of 4-alkylated isoquinoline derivatives in moderate to good yields. The σ-alkylpalladium(ii) intermediate in the Heck reaction activates alkynes toward intramolecular nucleophilic attack. This is the first example of a σ-alkylpalladium(ii) intermediate promoting the cyclization of alkynes containing a proximate nucleophilic center.
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