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Updated: Nov 2, 2025
![Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F60786.jpg&w=3840&q=50)
Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions
Published on: July 17, 2020
Synthesis of 2-Aryl-4H-thiochromen-4-one Derivatives via a Cross-Coupling Reaction
Peng Li1,2, Shengnan Li1, Gang Li1,2
1Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, 1 Xian Nong Tan Street, Beijing 100050, P. R. China.
Abstract:
A concise and efficient cross-coupling synthetic strategy has been developed to construct 2-aryl-4H-thiochromen-4-one derivatives from 2-sulfinyl-thiochromones and arylboronic acids. This reaction proceeds via a catalyst system of Lewis acid and palladium(II) combined with XPhos as an optimal ligand in moderate to good yields. Besides, this flexible methodology provides a wide scope for the synthesis of different functionally substituted thiochromone scaffolds and can be further exploited to construct diverse thioflavone libraries for pharmaceutical research.
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