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Synthesis of a unique dimethyl thiazoline containing intermediate of novel peroxisome proliferator-activated receptors(PPAR)δ agonists
- Man Kadayat, Tara, Lee, Geumwoo, Jung, Kyungjin, Hwang, Hee-Jong, Joo, Jeongmin, Hahn, Dongyup, Hwang, Hayoung, Park, Keun-Gyu, Cho, Sung Jin, Kim, Kyung-Hee, Chin, Jungwook
- Tetrahedron letters 2018 v.59 no.50 pp. 4384-4386
- agonists, chemical reactions, chemical structure, hyperlipidemia, metabolic syndrome, new drugs, peroxisome proliferator-activated receptors, tetrabutylammonium compounds
- Peroxisome proliferator-activated receptor delta (PPARδ) is considered as a promising biological target for the development of new drugs to treat metabolic syndrome including hyperlipidemia. In this study, a simple and efficient method for the preparation of a unique dimethyl thiazoline containing intermediate (13) of new PPARδ agonists as GW501516 analogue is described. The intermediate 13 was readily obtained by coupling reaction of 4-(chloromethyl)-5,5-dimethyl-2-(4-(trifluoromethyl)phenyl)-4,5-dihydrothiazole (11) with 4-mercapto-2-methylphenol (12) in the presence of tetrabutylammonium hydrogensulfate (TBAHS) and Cs2CO3 in DMF at 80 °C for 1 h. This unique intermediate could be useful for the synthesis of various novel PPARδ agonists to understand the structural and biological significance of PPARδ.