期刊
CHEMICAL SCIENCE
卷 11, 期 23, 页码 6070-6074出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0sc02439b
关键词
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资金
- Guangdong Natural Science Funds for Distinguished Young Scholar [2018B030306017]
- Guangdong Province Universities and Colleges Pearl River Scholar Funded Scheme (2018)
- National Natural Science Foundation of China [81602972]
- Fundamental Research Funds for the Central Universities [20ykzd15]
- Guangdong Provincial Key Laboratory of Chiral Molecule and Drug Discovery [2019B030301005]
Chemical modification of a specific amino acid residue on peptides represents an efficient strategy to improve their pharmacokinetics and facilitates the potential to achieve post-synthetic diversification of peptides. Herein, we reported the first Pd-catalyzed late-stageortho-olefination of Tyr residues on peptides with high chemo- and site-selectivity, by employing the easily attached and removable silanol as a bifunctional protecting group and directing group. Up to hexapeptides with variation on amino acid sequences or locations of the Tyr residue and different olefins were compatible with this protocol, which enriched the chemical toolbox for late-stage modificationviaC(sp(2))-H functionalization. Furthermore, the orthogonal protection strategies of Tyr were also developed and could be applied to SPPS.
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