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.

Abstract: This invention is directed to a new class of vitamin D compounds which are characterized by a modified ring A and triene structures and to a method for preparing same. The 7,8-dihydroxy-, 10.19-dihydroxy- and 10-oxo-19-nor-analogs of 25-hydroxyvitamin D.sub.3 are specifically disclosed.

Abstract: A process for preparing biologically active 1.alpha.-hydroxyvitamin D compounds from vitamin D compounds by hydroxylation at carbon 1 and subsequent photochemical isomerization, and novel intermediates and products resulting from this process are provided.

Abstract: The invention provides methods for preparing the various isomeric forms of 25-hydroxyvitamin D.sub.3 -26,23-lactone utilizing cyanohydrin formation with readily prepared steroid materials followed by actinic radiation of the products and recovery of the desired 25-hydroxyvitamin D.sub.3 -26,23-lactone.The invention also provides new intermediate compounds in their various isomeric forms derived during the process for preparing the said vitamin D.sub.3 lactones.25-Hydroxyvitamin D.sub.3 -26,23-lactone is recognized as having vitamin D-like activity and is believed to play an important role in the regulation of calcium and phosphate levels in the animal and human organism. The present invention provides a convenient method for preparing the various isomeric forms of this compound.

Abstract: The invention provides a method for chemically activating vitamin D compounds to obtain active rodenticidal preparations.The activated vitamin D preparation offers an effective and relatively inexpensive rodenticidal material.

Abstract: The invention provides a new vitamin D compound, 1.alpha.,25-dihydroxy-vitamin D.sub.3 26,23-lactone.The compound is characterized by vitamin D-like activity.

Abstract: A method for isotopically labeling carbon-6 of vitamin D and 5,6-trans-vitamin D compounds which comprises reducing the corresponding 6-oxo-cyclovitamin with a tritio- or deutero-borohydride and subjecting the reduction product to acid-catalyzed solvolysis.The 6-labeled compounds find application in the elucidation of vitamin D metabolism and function and in vitamin metabolite analyses.

Abstract: A method for preparing 1.alpha.-hydroxylated vitamin D compounds from 5,6-trans-vitamin D compounds which comprises allylically oxidizing a 5,6-trans-vitamin D compound, subjecting the oxidation product to actinic radiation in the presence of a photosensitizing agent and recovering the 1.alpha.-hydroxylated compound.1.alpha.-hydroxylation is recognized as being essential to impart biological activity to vitamin D compounds and their derivatives. The present invention provides an efficient method for maximizing the yield of 1.alpha.-hydroxylated vitamin D compounds.

Abstract: An improved method for the preparation of 1.alpha.-hydroxylated vitamin D compounds involving directly introducing an oxygen function at carbon 1 of the vitamin D molecule or precursors or derivatives thereof, wherein the 1.alpha.-hydroxycyclovitamin D intermediate is solvolyzed directly, without first converting the 1-hydroxy group to a 1-O-acyl function as a protective measure.

Abstract: A method for preparing 1.alpha.-hydroxyvitamin D compounds from 1.alpha.-hydroxy-3,5-cyclovitamin D compounds which comprises solvolyzing the 3,5-cyclovitamin D compound, exposing the solvolysis reaction products to actinic radiation in the presence of a photosensitizing agent and recovering the 1.alpha.-hydroxylated vitamin D compounds.1.alpha.-hydroxylation is recognized as being essential to impart biological activity to vitamin D compounds and their derivatives. The present invention provides an efficient method for maximizing the yield of 1.alpha.-hydroxylated vitamin D compounds.

Abstract: A method for directly introducing an oxygen function at carbon 1 of the vitamin D molecule or precursors of derivatives thereof which comprises subjecting such molecules to allylic oxidation utilizing selenium dioxide as the oxidizing agent.

Abstract: A method for directly introducing an oxygen function at carbon 1 of the vitamin D molecule or precursors or derivatives thereof which comprises subjecting such molecules to allylic oxidation utilizing selenium dioxide as the oxidizing agent.