Vitamin D3 derivative and its production method

Details Vitamin D3 derivative and its production method Vitamin D3 derivative and its production method

2006-01-03

2006-01-03

Qazi, Sabiha N. (Department: 1616)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

9,10-seco- cyclopentanohydrophenanthrene ring system doai

C552S653000

Reexamination Certificate

active

06982257

ABSTRACT:
Provided are 1,25-dihydroxy-2-methylvitamin D3 derivatives expressed by the general formula (I),[wherein each of R1and R2is independently a hydrogen atom or a tri(C1to C7alkyl)silyl group; herein configurations of asymmetric carbons at the 1-, 2- and 3-positions are each independently α-configuration or β-configuration] and their production methods.The compound is useful as a treating agent for osteoporosis, rickets, hyperthyroidism, etc.

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S. Nayeri et al; High-Affinity Nuclear Receptor Binding of 20-epi Analogues of 1,25-Dihydroxyvitamin D3 Correlates Well with Gene Activation; Feb. 2, 1996; pp. 325-333, J. of Cellular Biochemistry 62:325-333 (1996).
G. Posner et al; 2-Fluoroalkyl A-Ring Analogs of 1,25-Dihydroxyvitamin D3. Stereocontrolled Total Synthesis Via Intramolecular and Intermolecular Diels-Alder Cycloadditions, Preliminary Biological Testing; 1995; pp. 4617-4628; vol. 60; vol. 60, No. 14, J. Org. Chemistry.
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Katsuhiro Konno, et al.: “A Novel and Practical Route to A-Ring Enyne Synthon for 1α, 25-Dihydroxyvitamin D3Analogs: Synthesis of A-Ring Diastereomers of 1α, 25-Dihydroxyvitamin D3.” Bioorganic & Medicinal Chemistry Letters, vol. 8, No. 2, Jan. 20, 1998, p. 151-156. XP004136835.

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