Raed M. Al-Zoubi

Regioselective copper-catalyzed domino synthesis of 7-iodobenzo[d]oxazoles as potential ERβ ligands.

7-Halogenated benzoxazoles are a recurring motif in preclinical ligands for the estrogen receptor β (ERβ) and in other oxazole-based pharmacophores, yet selective and direct access to the 7-halo regiochemistry is not well served by classical condensation routes or by existing copper-catalyzed arylation methods. Here we...