Microwave-Assisted Ullmann C− S Bond Formation: Synthesis of the P38α MAPK Clinical Candidate VX-745

MC Bagley, T Davis, MC Dix, V Fusillo…

Index: Bagley, Mark C.; Davis, Terence; Dix, Matthew C.; Widdowson, Caroline S.; Kipling, David Organic and Biomolecular Chemistry, 2006 , vol. 4, # 22 p. 4158 - 4164

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Citation Number: 42

Abstract

Microwave irradiation promotes the rapid and efficient reaction of a thiophenol and aryl or heteroaryl halide using a copper or palladium catalyst and a range of ligands, depending upon substrate. Of particular utility is the use of copper (I) iodide (5 mol%) and trans- cyclohexane-1, 2-diol as ligand under basic conditions and microwave irradiation to give the corresponding sulfide in high yield. This method for C− S bond formation is applied in the ...