4.5 Article

Synthesis of the PPAR beta/delta-selective agonist GW501516 and C4-thiazole-substituted analogs

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 1, 页码 49-54

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.09.060

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thiazoles; Stille reactions; Suzuki reactions; nuclear receptors; PPAR

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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 PPAR beta/delta agonist yet described, and equally selective analogs at the thiazole-C4 position. (c) 2005 Elsevier Ltd. All rights reserved.

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