The third generation of aminobiphenyl palladacycle pre-catalyst "G3-Xantphos" enables functionalization of peptides containing cysteine in high yields. The conjugation (bioconjugation) occurs chemoselectively at room temperature under biocompatible conditions. Extension of the method to protein functionalization allows selective bioconjugation of the trastuzumab antibody.
Keywords: C−S bond-forming reaction; amino acids; antibody-drug conjugates; bioconjugation; palladium catalysis; peptides.
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