CHOLECALCIFEROLDERIVATER, DISSE DERIVATER TIL ANVENDELSE SOM TERAPEUTISK AKTIVE SUBSTANSER, FREMGANGSMAADE TIL FREMSTILLING AF DISSE, FARMACEUTISKE PRAEPARAT PAA BASIS AF DISSE, SAMT ANVENDELSE AF DISSE VED FREMSTILLING AF ET FARMACEUTISK PRAEPARAT

摘要

The 26,26,26-trifluoro-1 alpha ,25-dihydroxycholecalciferol, particularly the 26,26,26-trifluoro-1 alpha ,25R-dihydroxycholecalciferol essentially free of the 25S-epimer, and the 26,26,26-trifluoro-1 alpha ,25S-dihydroxycholecalciferol essentially free of the 25R-epimer, is prepared by reacting a compound of the formula wherein Y is trialkylated Si, with the carbanion of [3S-(3 alpha ,5 beta ,Z)]-2-[2-methylene-3,5-bis[(1,1 -dimethylethyl)dimethylsilyloxy]cyclohexylidene]-ethyldiphenyl phosphine oxide and removing the silyl protecting groups. It exhibits enhanced vitamin D3-like activity.