ChemInform Abstract: 11,21-Bisphenyl-19-norpregnane Derivatives are Selective Antiglucocorticoids.
Abstract
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ChemInform Abstract
An efficient eight-step synthesis of the title compounds (X) is described starting from dione (I). Key steps are the stereospecific Cu-catalyzed Grignard reaction to afford (VII) and the cross-coupling between the terminal alkyne (VII) and bromides (VIII). Screening of (X) and (XII) shows that specific combinations of polar substituents Ar and R lead to selective antiglucocorticoids.