Introducing glycans represents an efficient chemical
approach to
improve the pharmacological properties of therapeutic biomolecules.
Herein, we report an efficient synthesis of glycoconjugates through
chlorooxime–thiol conjugation. The reactive glycosyl chlorooximes,
derived from pyranoses or furanoses, readily couple to a wide range
of thiol-containing substrates, including peptides, sugars, and thiophenols.
This method features mild reaction conditions and fast kinetics. Capability
for aqueous media and gram-scale synthesis demonstrates the potential
of this method in the bioconjugation of saccharides with biologically
active molecules.