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Exploiting Aryl Mesylates and Tosylates in Catalytic Mono-α-arylation of Aryl- and Heteroarylketones

Wai Chung Fu, Chau Ming So, On Ying Yuen, Irene Toi Chuk Lee and Fuk Yee Kwong*

*State Key Laboratory of Chirosciences and Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, Email:

W. C. Fu, C. M. So, O. Y. Yuen, I. T. C. Lee, F. Y. Kwong, Org. Lett., 2016, 18, 1872-1875.

DOI: 10.1021/acs.orglett.6b00643


Enhanced steric congestion of an indolyl-derived phosphine ligand enables a Pd-catalyzed mono-α-arylation of aryl- and heteroarylketones with aryl mesylates and tosylates. This protocol is suitable for modifications of biological phenolic compounds, rendering it amenable for functionalization of phenolic (pro)drugs.

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ID: J54-Y2016