Chloride-Assisted Peptide Macrocyclization

Org Lett. 2020 Mar 20;22(6):2129-2134. doi: 10.1021/acs.orglett.0c00036. Epub 2020 Mar 10.


The role of the Cl- anion as a templating agent for the synthesis of cyclopeptides was assessed through the preparation of three new homocyclolysines and other six cyclic peptides by head-to-tail lactamization. Isolated yields of products obtained by chloride-templating approach were considerably higher than those gained by a cation-promoted procedure, whereby, in some cases, only the anion-assisted synthesis yielded the desired cyclopeptides.

Publication types

  • Research Support, Non-U.S. Gov't