Asymmetric synthesis of (2S,3S)-3-Me-glutamine and (R)-allo-threonine derivatives proper for solid-phase peptide coupling

Amino Acids. 2019 Mar;51(3):419-432. doi: 10.1007/s00726-018-2677-5. Epub 2018 Nov 17.

Abstract

Practical new routes for preparation of (2S,3S)-3-Me-glutamine and (R)-allo-threonine derivatives, the key structural components of cytotoxic marine peptides callipeltin O and Q, suitable for the Fmoc-SPPS, were developed. (2S,3S)-Fmoc-3-Me-Gln(Xan)-OH was synthesized via Michael addition reactions of Ni (II) complex of chiral Gly-Schiff base; while Fmoc-(R)-allo-Thr-OH was prepared using chiral Ni (II) complex-assisted α-epimerization methodology, starting form (S)-Thr(tBu)-OH.

Keywords: Asymmetric synthesis; Callipeltins; Epimerization; Michael additions; Tailor-made amino acids.

MeSH terms

  • Depsipeptides / chemistry*
  • Glutamine / chemistry*
  • Solid-Phase Synthesis Techniques / methods*
  • Stereoisomerism
  • Threonine / chemistry*

Substances

  • Depsipeptides
  • Glutamine
  • Threonine