“On water” direct Pd-catalysed C–H arylation of thiazolo[5,4-d]pyrimidine derivatives

Ye-Xiang Su; Ya-Hui Deng; Ting-Ting Ma; Yu-Yan Li; Li-Ping Sun

doi:10.1039/C2GC35399G

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Green Chemistry

Issue 7, 2012

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“On water” direct Pd-catalysed C–H arylation of thiazolo[5,4-d]pyrimidine derivatives

Ye-Xiang Su,^a Ya-Hui Deng,^a Ting-Ting Ma,^a Yu-Yan Li*^a and Li-Ping Sun*^a

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Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, P.R. China
E-mail: chslp@cpu.edu.cn ;
Fax: +(86)2583271351 ;
Tel: +(86)2583271445

Green Chem., 2012,14, 1979-1981

DOI: 10.1039/C2GC35399G
Received 19 Mar 2012, Accepted 26 Apr 2012
First published online 26 Apr 2012

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A novel protocol for the direct arylation of thiazolo[5,4-d]pyrimidine derivatives with aryl iodides is reported. The reactions were catalysed by a combination of Pd(PPh₃)₄ and Ag₂CO₃ (acting as the oxidant and the base as well), using exclusively water as the solvent and furnishing the desired products in good to excellent yields at only 60 °C.

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Ye-Xiang Su
Ya-Hui Deng
Ting-Ting Ma
Yu-Yan Li
Li-Ping Sun

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