Atropodiastereoselectivity in solid state BINOL synthesis: Leads from the estradiol platform

A novel functionalized steroidal BINOL scaffold is produced via a remarkable sequence of dehydrogenation, chlorination and atroposelective phenolic coupling steps. Its formation is straightforwardly obtained in a one-step synthesis under solid state conditions and in the absence of chiral additives.

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► Estradiol direct functionalization.
► One-step synthesis under solid state conditions.
► Atropostereoselective phenolic coupling.