Abstract: Disclosed is a method of preparing 2-hydroxy-3,17&bgr;-estradiol derivatives wherein 3,17&bgr;-estradiol is reacted with an organolithium reagent and reacted with either a boron reagent or a silicon reagent to form either a 2-boronyl or a 2-silyl modified estradiol analog represented by the corresponding structural formulae:
R1 and R2 are each independently a hydroxyl protecting group. R3, R4 and R5 are selected from the group consisting of halogens, alkyl, aryl, hydroxy, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl.
Abstract: This invention provides a novel synthesis and crystallization method and solvent for producing hexafluoro-vitamin D compounds, including 26, 26, 26, 27, 27, 27-hexafluoro-1.alpha., 25-dihydroxyvitamin D.sub.3. Crystalline forms of such compounds are provided that are especially suited for pharmaceutical use. Such compounds can exhibit biological activity for treating cancers, osteoporosis and psoriasis.
Abstract: 19-nor-vitamin D analog compounds and a method of synthesizing such compounds are disclosed. More particularly, examples of such compounds include 14-epi-19-nor-1.alpha.,25-dihydroxyvitamin D.sub.3, 14-epi-20-epi-19-nor-1.alpha., 25-dihydroxyvitamin D.sub.3, 14-epi-20-epi-19-nor-1.alpha.-hydroxyvitamin D.sub.3, 14-epi-19-nor-1.alpha., 25-dihydroxyvitamin D.sub.2, 14-epi-19-nor-24-homo-1.alpha., 25-didydroxyvitamin D.sub.3, 14-epi-19-nor-20(S)-hydroxymethyl-1.alpha.-hydropregnacalciferol, and 14-epi-19-nor-20(R)-hydroxymethyl-1.alpha.-hydroxypregnacalciferol.