Novel trifluorinated vitamin D3 intermediates
AssigneeHoffmann-La Roche Inc.
InventorsEnrico G. Baggiolini, Giacomo Pizzolato, Gary A. Truitt, Milan R. Uskovic
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Abstract
26,26,26-Trifluoro-1.alpha.,25-dihydroxy-cholecalciferol, and the 25R or 25S epimer thereof, are described, as well as processes and intermediates utilized to prepare the same, as well as pharmaceutical compositions containing the same. 26,26,26-trifluoro 1.alpha.,25-dihydroxycholecalciferol and the 25R or 25S epimer thereof are useful agents in the treatment of disease states such as osteoporosis, osteodystrophy and leukemia.
Claims6
A compound of the formula ##STR8## where X is aryl;
- and R.sub.1, R.sub.2 and R.sub.3 each independently are lower alkyl, aryl and aralkyl.
A process for producing 25-epimeric 26,26,26,-trifluoro-1.alpha.,25-dihydroxycholecalciferol which process comprises reacting a compound of the formula:
- ##STR9## where Y is alkyl and Z is R- or S- or an R,S-mixture with the carbanion of [3S-(3.alpha.,5.beta.,Z)]-2-[2-methylene-3,5-bis[(1.1-dimethylethyl)dimeth ylsilyloxy]cyclohexylidene]-ethyldiphenyl phosphine oxide and removing the silyl protecting groups.
A compound of the formula ##STR10## where Z is R-, S- or an R,S-mixture.
A compound of the formula ##STR11## where Y is alkyl and Z is R-, S- or an R,S-mixture.
Dependencies are inferred from the claim text.