4.7 Article

Solid-Phase Synthesis of Gly-Ψ[CH(CF3)NH]-Peptides

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 86, Issue 13, Pages 9225-9232

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.1c00853

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The solid-phase synthesis of Gly-Psi[CH(CF3)NH]-peptides has been developed, resulting in a small library of six peptidomimetics with high purity, analogues of biologically relevant peptides.
The solid-phase synthesis of Gly-Psi[CH(CF3)NH]-peptides is presented. In order to achieve this goal, the synthesis of Gly-Psi[CH(CF3)NH]-dipeptides having the C-terminus unprotected, the N-terminus protected as Fmoc- or Teoc-, and possibly side chain functionalities protected with acid-labile protecting groups has been developed. A selected small library of six peptidomimetics, encompassing analogues of biological relevant peptides, have been obtained in high purity.

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