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New heterocyclic retinoids/rexinoids exploiting halogen-selective cross-coupling reactions

Sequential Pd-catalyzed cross-coupling reactions of precursors dihalogenated heterocycles (thiazoles, thiophenes), using position-selective Stille or Suzuki coupling reactions, provided the scaffold for the synthesis of nuclear receptor modulators. In addition to several families of retinoids, compound GW501516, the most potent PPARd agonist yet described was also synthesized.

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UNIVERSIDADE DE VIGO
Oporto, 1
VIGO
Spain
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