- An improved synthesis of 24,24-difluoro-1α,25-dihydroxyvitamin D3 from readily available vitamin D2
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An improved synthesis of a highly potent vitamin D3 analog, 24,24-difluoro-1α,25-dihydroxyvitamin D3 (1b) has been accomplished via vitamin D2-SO2 adducts. The introduction of fluorine atoms was performed by tre
- Ando,Koike,Takayama
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p. 189 - 192
(2007/10/02)
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- An improved synthesis of 24,24-difluoro-1α,25-dihydroxy-vitamin D3 from vitamin D2
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An improved synthesis of a highly potent vitamin D3 analog, 24,24-difluoro-1α,25-dihydroxyvitamin D3 has been accomplished. The total yield was 9.3% from inexpensive vitamin D2 in 11 steps.
- Ando,Kondo,Koike,Takayama
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p. 1662 - 1664
(2007/10/02)
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- An alternative and efficient synthesis of 24,24-difluoro-1α,25-dihydroxyvitamin D3
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An alternative synthesis of the title compound 2, a highly potent analog of 1α,25-dihydroxyvitamin D3 (1), is described. Starting with 1α,3β-bis[(tert-butyldimethylsilyl)oxy]androst-5-ene (8), 2 was obtained in 3.8% total yield through 10 steps. This method provides compound 2 in much higher yield than that reported previously.
- Konno,Ojima,Hayashi,Takayama
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p. 1120 - 1124
(2007/10/02)
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- Immunosuppressive agents
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The invention relates to pharmaceutical compositions comprising at least one Vitamin D derivative and a method of using the pharmaceutical compositions in suppressing immune responses.
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- Process for the preparation of 24,24-difluoro-1α,25-dihydroxy vitamin D3 and intermediates obtained therefrom
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The present invention relates to a process and intermediates for the preparation of 24,24-difluoro-1α,25-dihydroxycholecalciferol from the readily-available 1α,3β-dihydroxyandrost-5-en-17-one which is made by a known microbiological process from 3β-hydroxyandrost-5-en-17-one [R. M. Dodson, A. H. Goldkamp and R. D. Muir, J. Amer. Chem. Soc. 82 4026 (1960)].
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- Method of treatment
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The present invention relates to a method of treating osteoporosis by administering to a host suffering from osteoporosis an effective amount of 24,24-difluoro-1α,25-dihydroxycholecalciferol.
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