Selective Antiglucocorticoids.-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.-(GEBHARD, R.; VAN DER VOORT, H.; SCHUTS, W.; SCHOONEN, W.; Bioorg. Med. Chem. Lett. 7 (1997) 17, 2229-2234 Sci. Dev. Group, Organon Int. BV, NL-5340 BH Oss, Neth.; EN)
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