A radical cyclization approach to the formal total syntheses of platencin

Org Biomol Chem. 2011 Oct 26;9(22):7877-86. doi: 10.1039/c1ob06155k. Epub 2011 Oct 3.

Abstract

Two different strategies leading to formal total syntheses of platencin are described. The first strategy involving Claisen rearrangement and radical cyclization provides a rapid access to the core structure of platencin, and also use minimum protective-group operations. The second strategy, a protecting group-free route, utilizes a 6-exo-trig radical cyclization and aldol condensation as key steps leading to the formal synthesis of platencin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3-Oxoacyl-(Acyl-Carrier-Protein) Synthase
  • Acetyltransferases / antagonists & inhibitors*
  • Acetyltransferases / metabolism
  • Aminophenols / analysis
  • Aminophenols / chemical synthesis*
  • Aminophenols / pharmacology
  • Anti-Bacterial Agents / analysis
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Bacteria / drug effects
  • Bacteria / enzymology
  • Bacterial Infections / drug therapy
  • Bacterial Infections / microbiology
  • Chemistry, Pharmaceutical / methods*
  • Cyclization
  • Drug Discovery
  • Escherichia coli Proteins / antagonists & inhibitors*
  • Escherichia coli Proteins / metabolism
  • Fatty Acid Synthase, Type II / antagonists & inhibitors
  • Fatty Acid Synthase, Type II / metabolism
  • Fatty Acids / metabolism
  • Free Radicals / chemistry
  • Humans
  • Lipid Metabolism / drug effects
  • Molecular Structure
  • Polycyclic Compounds / analysis
  • Polycyclic Compounds / chemical synthesis*
  • Polycyclic Compounds / pharmacology
  • Stereoisomerism

Substances

  • Aminophenols
  • Anti-Bacterial Agents
  • Escherichia coli Proteins
  • Fatty Acids
  • Free Radicals
  • Polycyclic Compounds
  • Acetyltransferases
  • fabH protein, E coli
  • 3-Oxoacyl-(Acyl-Carrier-Protein) Synthase
  • Fatty Acid Synthase, Type II
  • platencin