Asymmetric synthesis of (S)-α-(octyl)glycine via alkylation of Ni(II) complex of chiral glycine Schiff base

Chirality. 2020 Dec;32(12):1354-1360. doi: 10.1002/chir.23281.

Abstract

Over last decade, the use of Ni(II) complexes, derived from of glycine Schiff bases with chiral tridentate ligands, has emerge as a leading methodology for preparation of structurally diverse Tailor-Made Amino Acids, the key structural units in modern medicinal chemistry, and drug design. Here, we report asymmetric synthesis of derivatives of (S)-α-(octyl)glycine ((S)-2-aminodecanoic acid) and its N-Fmoc derivative via alkylation of chiral nucleophilic glycine equivalent with n-octyl bromide. Under the optimized conditions, the alkylation proceeds with excellent yield (98.1%) and diastereoselectivity (98.8% de). The observed stereochemical outcome and convenient reaction conditions bode well for application of this method for large-scale asymmetric synthesis of (S)-2-aminodecanoic acid and its derivatives.

Keywords: Schiff bases; Tailor-Made Amino Acids™; amino acids; asymmetric synthesis; chiral tridentate ligands; square-planar Ni(II) complexes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Chemistry Techniques, Synthetic
  • Coordination Complexes / chemistry
  • Glycine / chemistry*
  • Molecular Structure
  • Nickel / chemistry*
  • Schiff Bases / chemistry*
  • Stereoisomerism

Substances

  • Coordination Complexes
  • Schiff Bases
  • Nickel
  • Glycine