Highly Diastereoselective Synthesis of a HCV NS5B Nucleoside Polymerase Inhibitor

J Org Chem. 2019 Apr 19;84(8):4780-4795. doi: 10.1021/acs.joc.8b02500. Epub 2018 Dec 10.

Abstract

An asymmetric synthesis of HCV NS5B nucleoside polymerase inhibitor (1) is described. This novel route features several remarkably diastereoselective and high-yielding transformations, including construction of the all-carbon quaternary stereogenic center at C-2 via a thermodynamic aldol reaction. A subsequent glycosylation reaction with activated uracil via C-1 phosphate and installation of the cyclic phosphate group using an achiral phosphorus(III) reagent followed by oxidation provides 1.

MeSH terms

  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Hepacivirus / drug effects
  • Hepatitis C, Chronic / drug therapy
  • Humans
  • Molecular Structure
  • Stereoisomerism
  • Viral Nonstructural Proteins / antagonists & inhibitors*
  • Viral Nonstructural Proteins / metabolism

Substances

  • Antiviral Agents
  • Viral Nonstructural Proteins
  • NS-5 protein, hepatitis C virus