A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta

  • J Org Chem. 2003 Nov 14;68(23):9116-8. doi: 10.1021/jo035140g.
Zhi-Liang Wei  1 ,  Alan P Kozikowski
Affiliations
  • 1. Drug Discovery Program, Department of Neurology, Georgetown University Medical Center, 3900 Reservoir Road NW, Washington, D.C. 20057, USA.
PMID: 14604391 DOI: 10.1021/jo035140g
Abstract

The most potent and selective Peroxisome Proliferator-activated Receptor delta (PPARdelta) agonist GW501516 (1) was synthesized in 4 steps and 78% overall yield starting from o-cresol by using a one-pot regiocontrolled dialkylation of mercaptophenol 5 as the key step.

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