ChemInform Abstract: Biphenylsulfonamide Endothelin Receptor Antagonists. Part 3. Structure—Activity Relationship of 4′‐Heterocyclic Biphenylsulfonamides.

Abstract

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Metal‐Free Hypervalent‐Iodine‐Promoted C3 Difluorination and C2 Oxidation of N‐Substituted Indoles

“…Introduction of fluorine atoms into the skeletons of oxindoles has attracted much attention from organic chemists and medicinal chemists, because this transformation significantly changes the physical, chemical and biological properties, compared to their parent non‐fluorinated oxindoles, often to an advantage . For example, compound 1 is a potent and selective EP3 receptor antagonist; compound 2 inhibits the activity of endothelin and is useful as an antihypertensive; compound 3 has anticancer activity; compound 4 was tested as a preventive and therapeutic agent for nervous system disorders; compound 5 could act as an ErbB kinase inhibitor (Figure ). The key feature of these biologically active compounds is that they possess a 3,3‐difluoro‐2‐oxindole subunit.…”