Chemoselective Peptide Cyclization and Bicyclization Directly on Unprotected Peptides

26 June 2019, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

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.

Keywords

peptide cyclization

Supplementary materials

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OPA cyclization-JACS20190530
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