P(III) vs P(V): A P(V) Reagent for Thiophosphoramidate Linkages and Application to an Asymmetric Synthesis of a Cyclic Dinucleotide STING Agonist

J Org Chem. 2022 Feb 18;87(4):1934-1940. doi: 10.1021/acs.joc.1c01055. Epub 2021 Jul 7.

Abstract

A highly stereoselective synthesis of a cyclic dinucleotide (CDN) STING agonist containing two chiral thiophosphoramidate linkages is described. These rare yet key functional groups were, for the first time, installed efficiently and with high diastereoselectivity using a specially designed P(V) reagent. By utilizing this strategy, the CDN was prepared in greater than 16-fold higher yield than the prior P(III) approach, with fewer hazardous reagents and chromatographic purifications.

MeSH terms

  • Indicators and Reagents
  • Membrane Proteins* / chemistry

Substances

  • Indicators and Reagents
  • Membrane Proteins