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Updated: Jan 18, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Cs2CO3-Catalyzed Decarboxylation/Cyclization to Access Functionalized 8-Hydroxyisoquinoline-1(2H)-ones and
Weiqiang Li1,2, Lifeng Yao3, Guiyun Zeng1
1National and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, School of Chemistry and Environment, Yunnan Minzu University, Kunming 650500, P. R. China.
Abstract:
We herein describe a novel decarboxylation/cyclization sequence involving a three-component reaction of dialkyl 2-(alkoxymethylene)malonate, amines, and terminal alkyne ester or internal alkyne ester catalyzed by Cs2CO3 under microwave conditions. These two types of highly chemo- and regioselective transformations were accomplished by different reaction channels to furnish a wide range of functionalized 8-hydroxyisoquinoline-1(2H)-ones (21 examples) and 2-pyridones (18 examples) in good to excellent yields and might provide new opportunities for the discovery of N-heterocyclic drugs and other functional molecules.
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