Abstract

The hydantoin moiety is an important structural motif present in various pharmaceuticals. Palladium complexes bearing electron-rich, bulky ylide-functionalized phosphine (YPhos) ligands were found to catalyze the arylation of N-protected hydantoins with broadly available aryl chlorides. Selective monoarylations, sequential diarylations, and arylation-alkylation sequences have been achieved. In combination with stepwise deprotection strategies, this opens up an expedient access to a wide variety of hydantoins, including derivatives of the anticonvulsant drugs phenytoin and mephenytoin.

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