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Pyridinesulfinates, Pyrimidinesulfinates [Cross-coupling Reaction using Transition Metal Catalysts]

Pyridine-2-sulfinates and pyrimidine-2-sulfinates can be utilized in Suzuki-Miyaura cross coupling reagents as replacements for pyridine-2-boronic acids and pyrimidine-2-boronic acids, which are difficult to prepare. These reagents are tolerated by ketone, ester, trifluoromethyl, and other functional groups.1,2) Also the cross-coupling reaction with Grignard reagents proceeds without transition metals.3) It has been reported that these reagents are applied to late-stage modifications in drug discovery, and ligand syntheses for catalytic reactions.

References
- 1)Pyridine sulfinates as general nucleophilic coupling partners in palladium-catalyzed cross-coupling reactions with aryl halides
- 2)Desulfination as an Emerging Strategy in Palladium‐Catalyzed C–C Coupling Reactions
- 3)Transition-Metal-Free Desulfinative Cross-Coupling of Heteroaryl Sulfinates with Grignard Reagents