A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta.
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.
Wei
Zhi-Liang
ZL
Drug Discovery Program, Department of Neurology, Georgetown University Medical Center, 3900 Reservoir Road NW, Washington, D.C. 20057, USA.
Kozikowski
Alan P
AP
D009682:Magnetic Resonance Spectroscopy; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014157:Transcription Factors / Q000819:agonists*
C425931:GW 501516; D018160:Receptors, Cytoplasmic and Nuclear; D013844:Thiazoles; D014157:Transcription Factors