The auxiliary-assisted, palladium-catalyzed functionalization of acid derivatives was used to modify �-positions of amino acids. Efficient methods were developed for acetoxylation, arylation, and alkylation of amino acid C-H bonds. Good functional group tolerance was observed. Moreover, the auxiliary can be removed in one step to generate the modified amino acids in high yield and with minimal erosion of enantiomeric excess.

Unnatural amino acid synthesis By C-H bond functionalization methodology

243rd National Meeting (2012)

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