Fluorovitamin D compounds and processes for their preparation
AssigneeWisconsin Alumni Research Foundation
InventorsHector F. DeLuca, Heinrich K. Schnoes, Joseph L. Napoli, Jr., Bruce L. Onisko
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Abstract
Fluorine-substituted vitamin D compounds, methods for preparation of such compounds and fluorinated intermediate compounds used in such methods are disclosed. The fluorine-substituted vitamin D compounds are characterized by vitamin D-like activity in stimulating intestinal calcium transport and bone mobilization and in promoting the calcification of rachitic bone.
Claims9
Compounds having the formula ##STR6## where R.sub.1 is selected from the group consisting of hydrogen, hydroxy, O-acyl and O-lower-alkyl,
- R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are each selected from the group consisting of hydrogen, hydroxy, O-acyl, O-lower-alkyl and fluoro, except that at least one of R.sub.2, R.sub.3, R.sub.4, and R.sub.5 must be fluoro, and
- R.sub.6 is hydrogen or lower alkyl.
1-fluoro-5,6-trans-vitamin D.sub.3.
1-Fluoro-25-hydroxy-5,6-trans-vitamin D.sub.3.
1,25-difluoro-5,6-trans-vitamin D.sub.3.
25-fluoro-5,6-trans-vitamin D.sub.3.
24-hydroxy-25-fluoro-5,6-trans-vitamin D.sub.3.
1.alpha.-hydroxy-25-fluoro-5,6-trans-vitamin D.sub.3.
1.alpha.,24(R)-dihydroxy-25-fluoro-5,6-trans-vitamin D.sub.3.
Dependencies are inferred from the claim text.