Abstract
Cyclic peptides are an important class of bioactive compounds for the chemical biology and pharmaceutical industry. Chemical synthesis of highly constrained cyclic peptides is often challenging. Here we describe the synthetic strategy of peptide macrocyclization through late-stage palladium-catalyzed C-H activation. These methods utilize endogenous backbone amides in the peptide sequence as directing groups and are efficient in the preparation of small-to-middle size peptide macrocycles.
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Acknowledgments
This work is supported by NSF of China (Grant 21922703 and 91953112), the Natural Science Foundation of Jiangsu Province (Grant BK20190004) and the Fundamental Research Funds for the Central Universities (Grant 14380138 and 14380131).
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Cai, C., Liu, S., Wang, H. (2022). Peptide Macrocyclization Through Palladium-Catalyzed Late-Stage C-H Activation. In: Coppock, M.B., Winton, A.J. (eds) Peptide Macrocycles. Methods in Molecular Biology, vol 2371. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-1689-5_3
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DOI: https://doi.org/10.1007/978-1-0716-1689-5_3
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