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.
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“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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