Ortho-Directed Palladium-Catalyzed Direct C–H Functionalization of 3-Picolinyl- and 3-(2-Cyanoethyl)pyrimidin-4(3H)-ones with Aryl Halides
Résumé
The ortho-directed palladium-catalyzed direct C-H arylation of N-picolinyl pyrimidin-4-one was achieved with various aryl halides. The methodology was extended towards C-H arylation of pyrimidin-4-ones incorporating methoxy group and aryl groups at C5 site. The 2cyanoethyl was also evaluated as ortho-directed group. The methodology gives access to innovative N-substituted 2-and 2,5-diarylated pyrimidin-4-ones. The standard 3-step deprotection sequence of picolinyl group was also studied.
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