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Chinese scientists have developed a new method for synthesising 2-arylsubstituted thiazolo[5,4-d]pyrimidine derivatives under mild conditions.

2-Arylsubstituted thiazolo[5,4-d]pyrimidine derivatives are the main motif in many pharmacologically relevant compounds including Tie-2 inhibitors and immunosuppressive agents.  Given the interest in these compounds, finding a mild and effective route to synthesis them is important.  Existing methods involve the use of toxic reagents and harsh conditions which limit their applications.  In this work, Tu-Yan Li, Li-Ping Sun and colleagues from China Pharmaceutical University, Nanjing, China, have developed a procedure for the direct arylation of thiazolo[5,4-d]pyrimidine derivatives with aryl iodides.  They employ a combination of Pd(Ph3)4 and Ag2CO3 used exclusively in water at 60 °C, giving the products in good to excellent yields.

This article is free to access until the 6th July 2012!  Click on the link below to find out more…

“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 and Li-Ping Sun, Green Chem., 2012, DOI: 10.1039/C2GC35399G

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