Synthesis of 4,6-disubstituted 2-(4-morpholinyl)pyrimidines by cross-coupling reactions using triorganoindium compounds.

Martínez, M. M.; Pérez-Caaveiro, C.; Peña-López, M.; Sarandeses, L. A.; Pérez Sestelo, J.


Org. Biomol. Chem. 2012, 10, 9045–9051 (DOI: 10.1039/c2ob26398j).

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4,6-Disubstituted-2-(4-morpholinyl)pyrimidines, an important class of bioactive compounds, have been synthesized from 4,6-dichloro-2-(4-morpholinyl)pyrimidine by selective and sequential palladium catalyzed cross-coupling reactions using triorganoindium reagents. This methodology, being efficient and versatile, allowed the synthesis of a variety of non-symmetrical pyrimidines functionalized at C-4 and C-6 positions.