Tetrahedron Letters p. 1882 - 1884 (2016)
Update date:2022-07-29
Topics: Synthetic route Versatility Safety Considerations Research and Synthesis
O'Donnell, Michael
Charrier, Jean-Damien
A novel synthetic route to 2,4-functionalized pyrimidines is reported. The approach uses 2-chloro-4-tetrafluorophenoxypyrimidine, that enables sequential palladium catalyzed functionalization at the pyrimidine C-2 position, followed by SNAr displacement with diverse amines at C-4. The broad utility of this 'C-2 then C-4' functionalization sequence has been demonstrated with a range of cross-coupling partners and amines.
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