A Stereospecific Synthesis of (2 S,3 R)-β-Methyltryptophans

Org Lett. 2026 Jun 19;28(24):7833-7838. doi: 10.1021/acs.orglett.6c02033. Epub 2026 Jun 5.

Abstract

The surging demand for novel tryptophan analogues across small-molecule, bioactive peptide, and conjugate therapeutic modalities underscores an unmet synthetic need for efficient access to (2S,3R)-β-methyltryptophans. Herein, we describe a practical and stereospecific synthesis of (2S,3R)-β-methyltryptophans that offers broad functional group compatibility and structural diversity.

MeSH terms

  • Molecular Structure
  • Stereoisomerism
  • Tryptophan* / analogs & derivatives
  • Tryptophan* / chemical synthesis
  • Tryptophan* / chemistry

Substances

  • Tryptophan