Late-Stage Diversification of Imidazole-Based Pharmaceuticals through Pd-Catalyzed Regioselective C-H Bond Arylations
Résumé
Palladium-catalyzed C-H bond arylation of imidazoles has been applied to pharmaceuticals such as Bifonazole, Climbazole, and Prochloraz. In the presence of phosphine-free Pd(OAc)(2) catalyst, aryl bromides are efficiently coupled at the CS-position of the imidazole units, which are widely decorated. Under these conditions, only C-H bond arylation reaction occurred without affecting the integrity of chemical structure of the imidazole-based pharmaceuticals. Moreover, with Bifonazole Pd-catalyzed C-H bond diarylation at the C2- and C5-positions of imidazole unit has also been performed.
Fichier principal
Soule_et al_2019_Late-Stage Diversification of Imidazole-Based Pharmaceuticals_accepted.pdf (2 Mo)
Télécharger le fichier
Origine | Fichiers produits par l'(les) auteur(s) |
---|
Loading...