4.7 Article

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

期刊

JOURNAL OF ORGANIC CHEMISTRY
卷 74, 期 21, 页码 8336-8342

出版社

AMER CHEMICAL SOC
DOI: 10.1021/jo9017155

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资金

  1. Engineering and Physical Sciences Research Council [GR/S25456]
  2. Biotechnology and Biological Sciences Research Council [BB/D524140/1]
  3. SPARC
  4. Biotechnology and Biological Sciences Research Council [BB/D524140/1] Funding Source: researchfish
  5. BBSRC [BB/D524140/1] Funding Source: UKRI

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Microwave irradiation promotes the rapid and efficient reaction of I thiophenol and aryl or heteroaryl halide using it copper or palladium catalyst and it 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 four-step synthesis of the clinical candidate VX-745 in 38% over-all yield. The inhibitory activity of VX-745 against p38 alpha MAPK is confirmed in Werner syndrome dermal fibroblasts at 1.0 mu M concentration by immunoblot assay

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