Microwave-assisted, efficient and regioselective Pd-catalyzed C-phenylation of halopyrimidines

作者：Ceide Susana Conde; Montalban Antonio Garrido^*

来源：Tetrahedron Letters, 2006, 47(26): 4415-4418.

DOI：10.1016/j.tetlet.2006.04.082

• microwave
• palladium
• cross-coupling
• heterocycles
• regioselectivity

We herein report that flash heating microwave irradiation is a helpful tool in the formation of arylpyrimidines from the corresponding halopyrimidines. The palladium-catalyzed cross-coupling reactions of 2,4-di- and 2,4,5-trihalopyrimidines with phenoylboronic acid under the above conditions are described. By use of the appropriate catalyst and the adequate halopyrimidine, good regioselectivity can be achieved in the 2-, 4-, or 5-positions of the heterocycle. In addition, we show that this methodology, is ameneable for the stepwise preparation of mono-, di-, and triphenylpyrinlidines.

• 出版日期2006-6-26