Patent Number: 6,251,883

Title: Methods for preparation and use of 1.alpha.,24(S)-dihydroxy vitamin D2

Abstract: 1.alpha.,24(S)-Dihydroxy vitamin D.sub.2 which is useful as an active compound of pharmaceutical compositions for the treatment of disorders of calcium metabolism and for various skin disorders. The invention also includes preparation of synthetic 1.alpha.,24(S)-dihydroxy vitamin D.sub.2 starting from ergosterol which is converted in six steps to 24-hydroxyergosterol. 24-Hydroxyergosterol is irradiated and thermally converted to 24-hydroxy vitamin D.sub.2 which is converted in six steps to 1.alpha.,24(S)-dihydroxy vitamin D.sub.2. The syntheses also produced novel intermediates.

Inventors: Horst; Ronald L. (Ames, IA), Bishop; Charles W. (Madison, WI), Jones; Glenville (Kingston, CA), Koszewski; Nicholas J. (Lexington, KY), Knutson; Joyce C. (Madison, WI), Moriarty; Robert M. (Oak Park, IL), Reinhardt; Timothy (Ames, IA), Penmasta; Raju (Westmount, IL), Strugnell; Stephen (Madison, WI), Guo; Liang (Bolingbrook, IL), Singhal; Sanjay K. (Morton Grove, IL), Zhao; Lei (Lamont, IL)

Assignee: Bone Care International, Inc.

International Classification: A61K 31/59 (20060101); A61K 45/00 (20060101); A61K 45/06 (20060101); C07C 401/00 (20060101); C07J 9/00 (20060101); C07J 71/00 (20060101); A01N 045/00 (); A61K 031/59 ()

Expiration Date: 06/26/2018