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Through the synergistic catalytic effect of the halogen bond (XB) donor and thiourea catalyst, a direct α-selective N-glycosylation of the amide residue of asparagine derivative was achieved using readily accessible glycosyl trichloroacetimidate. n-Butyl methyl ether was found to be the most suitable solvent for the α-selectivity.

Organocatalytic Direct α-Selective <i>N</i>-Glycosylation of Amide with Glycosyl Trichloroacetimidate