3 years ago

Solid-Phase Synthesis of Oxetane Modified Peptides

Solid-Phase Synthesis of Oxetane Modified Peptides
Jonathan D. Beadle, Alex Hoose, Astrid Knuhtsen, Michael Shipman, Andrew G. Jamieson, Piotr Raubo
Solid-phase peptide synthesis (SPPS) is used to create peptidomimetics in which one of the backbone amide C═O bonds is replaced by a four-membered oxetane ring. The oxetane containing dipeptide building blocks are made in three steps in solution, then integrated into peptide chains by conventional Fmoc SPPS. This methodology is used to make a range of peptides in high purity including backbone modified derivatives of the nonapeptide bradykinin and Met- and Leu-enkephalin.

Publisher URL: http://dx.doi.org/10.1021/acs.orglett.7b01466

DOI: 10.1021/acs.orglett.7b01466

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