HBTM-2.1 promotes the direct asymmetric α-amination of carboxylic acids with N-aryl-N-aroyldiazenes at low catalyst loadings (as low as 0.25 mol%), giving either 1,3,4-oxadiazin-6-ones or N-protected α-amino acid derivatives (upon ring opening) with exquisite enantiocontrol (typically ≥99% ee).
Chemical Science
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