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Chemoselective Peptide Cyclization and Bicyclization Directly on Unprotected Peptides

preprint
submitted on 25.06.2019 and posted on 26.06.2019 by Yue Zhang, Qing Zhang, Clarence Wong, Xuechen Li
Herein, we report a highly chemoselective and operation-simple method directly cyclizing unprotected peptides, in which ortho-phthalaldehyde (OPA) is found to react with the lysine/N-terminus and cysteine within one unprotected peptide sequence effectively to form the isoindole-bridged cyclic peptides. This reaction is carried out in the aqueous buffer and features tolerance of diverse functionalities, rapid and clean transformation and operational simplicity.

Funding

University Grants Committee

History

Email Address of Submitting Author

xuechenl@hku.hk

Institution

The University of Hong Kong

Country

China, Hong Kong

ORCID For Submitting Author

0000-0001-5465-7727

Declaration of Conflict of Interest

a patent filed

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in Journal of the American Chemical Society

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