Palladium-catalyzed regioselective C-5 arylation of protected l-histidine: Microwave-assisted C-H activation adjacent to donor arm

摘要

An efficient, microwave-assisted direct C-H arylation at the C-5 position of fully protected l-histidine has been achieved via a palladium-catalyzed transformation reaction. This highly regioselective reaction has been applied to synthesize a series of protected 5-aryl-l-histidines using aryl iodides as coupling partners, in good to excellent yields. The reaction is compatible with substrates possessing electron-donating or electron-withdrawing substituents and offers high reactive functional group tolerance.