Synthesis of the PPARβ/δ-selective agonist GW501516 and C4-thiazole-substituted analogs

Sequential, position-selective, Pd-catalyzed cross-coupling reactions of 2,4-dibromo-5-hydroxymethylthiazole provided the scaffold for the synthesis of GW501516, the most potent PPARβ/δ agonist yet described, and equally selective analogs at the thiazole-C4 position.

Figure optionsDownload as PowerPoint slide