Nickel-catalyzed and Li-mediated regiospecific C-H arylation of benzothiophenes
Résumé
A nickel-based catalytic system for the regiospecific C2-H arylation of benzothiophene has been established. NiCl2(bpy) is used as catalyst in combination with LiHMDS as base in dioxane. The catalytic system is applicable to a variety of funtionalized benzothiophenes, as well as other heteroarenes including thiophene, benzodithiophene, benzofuran and selenophene in combination with iodo aryl electrophiles. The role of LiHMDS as uniquely potent base and a postulated mechanism are discussed. The applicability of this system is finally demonstrated for the synthesis of an intermediate of anactive pharmaceutical ingredient.
Origine : Fichiers produits par l'(les) auteur(s)
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