期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 56, 期 12, 页码 3177-3181出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201611202
关键词
bioconjugation; chemoselectivity; cross-coupling; peptide macrocyclization; phosphane ligands
资金
- Merck Co.
- National Institutes of Health [R01GM110535]
A mild method for the arylation of lysine in an unprotected peptide is presented. In the presence of a preformed biarylphosphine-supported palladium(II)-aryl complex and a weak base, lysine amino groups underwent C-N bond formation at room temperature. The process generally exhibited high selectivity for lysine over other amino acids containing nucleophilic side chains and was applicable to the conjugation of a variety of organic compounds, including complex drug molecules, with an array of peptides. Finally, this method was also successfully applied to the formation of cyclic peptides by macrocyclization.
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