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Preparation of 3-Acyl-4-arylcoumarins via Metal-Free Tandem Oxidative Acylation/Cyclization between Alkynoates with Aldehydes

Xia Mi, Chenyang Wang, Mengmeng Huang*, Yusheng Wu* and Yangjie Wu

*College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450052; Tetranov Biopharm, LLC, 75 Daxue Road, Zhengzhou 450052, P.R. China, Email:,

X. Mi, C. Wang, M. Huang, Y. Wu, Y. Wu, J. Org. Chem., 2015, 80, 148-155.

DOI: 10.1021/jo502220b (free Supporting Information)


An efficient metal-free tandem acylation/cyclization of alkynoates with aldehydes enables the synthesis of 3-acyl-4-arylcoumarins via addition of acyl radical to alkynes and a C-H bond functionalization to form two new C-C bonds simultaneously.

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Key Words

Coumarins, Potassium peroxydisulfate

ID: J42-Y2015