- Degree-of-freedom alcohol and preparation method thereof
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The invention provides alcidol and a preparation method thereof, and the preparation method comprises the following steps: D. 2 The initial material is subjected to a sulfonylation reaction in sequence. The methoxy - is reacted with a bridging
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Paragraph 0051-0055; 0080-0084; 0112-0116
(2021/11/21)
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- Based on nitrogen heterocyclic modified vitamin D2 derivatives, synthesis and use
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The invention discloses a vitamin D2 derivative modified by N-heterocycle, as well as synthesis and application of the vitamin D2 derivative. The vitamin D2 derivative is synthesized through the following steps: taking vitamin D2 as a raw material, and co
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Paragraph 0021; 0024; 0025; 0026
(2017/08/25)
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- STABILIZED DOXERCALCIFEROL AND PROCESS FOR MANUFACTURING THE SAME
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1 a-hydroxy vitamin D2 (doxercalciferol) of exceptionally high purity and stability is prepared by a process involving chromatographically purifying 1 α-hydroxyvitamin D2 monoacetate, chemically removing the acetate protectant group
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Page/Page column 5; 6
(2011/10/13)
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- METHODS FOR PRODUCING PARICALCITOL
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The present invention is directed to novel processes for the preparation of paricalcitol to novel intermediates used in these processes, and to processes for preparation of the novel intermediates.
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Page/Page column 100
(2010/04/03)
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- Process for preparation of paricalcitol and intermediates thereof
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The invention relates to a novel process for the preparation of Paricalcitol and intermediates thereof.
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Page/Page column 10-11; Sheet 1/2
(2009/03/07)
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- PROCESS FOR PREPARATION OF PARICALCITOL INTERMEDIATES
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The present invention relates to a compound and a novel process for the preparation of Paricalcitol intermediates.
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Page/Page column 5
(2009/12/28)
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- Convenient synthesis of 1α,25-dihydroxyvitamin D3 from vitamin D2
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(1S,6R)-1-Acetoxy-6-(1,3-benzodithiol-2-yloxy)-3,5-cyclovitamin D2 (7) was synthesized from vitamin D2 by five steps. The new compound 7 was ozonized regioselectively and subsequently reduced, leading to (7E)-(1S,3S,5R,6R)-1-acetoxy-6-(1,3-benzodithiol-2-yloxy)-3,5-cyclo-9, 10-seco-23,24-dinor-7,10(19)-choladien-22-ol (11). The alcohol 11 obtained as a key intermediate was tosylated, iodinated, and coupled with 2-methyl-4-phenylsulfonyl-2-(tetrahydropyranyloxy)butane to give (1S,6R)-1-hydroxy-6-(1,3-benzodithiol-2-yloxy)-23-phenylsulfonyl-25-te trahydropyranyloxy-3,5-cyclovitamin D3 (16). By desulfonylation and hydrolysis of the compound 16 1α,25-dihydroxyvitamin D3 was obtained selectively.
- Takahashi,Sakakibara
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p. 2494 - 2499
(2007/10/02)
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- SYNTHESIS OF (24R)-24,25-DIHYDROXYVITAMIN D3
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Two versions of the stereoselective synthesis of (24R)-24,25-dihydroxyvitamin D3 were realized.Vitamin D2 and ergosterol were used as starting materials.Methods are proposed for the production of the following key compounds: 6-Methoxy-23,24-bisnor-9,10-seco-3,5-cyclochola-7,10(19)-dien-22-yl phenyl sulfone; 3β-hydroxy-23,24-bisnorchola-5,7-dien-22-yl phenyl sulfone; (2R)-3-methylbutane-1,2,3-triol 1-p-toluenesulfonate.
- Bogoslovskii, N. A.,Samokhvalova, N. G.,Isaeva, T. A.,Valashek, I. E.,Filippova, T. M.,Kharchevnikov, A. P.
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p. 2070 - 2081
(2007/10/02)
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- Direct C(1) Hydroxylation of Vitamin D3 and Related Compounds
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A direct synthesis of C(1) hydroxylated vitamin D analogues from the corresponding vitamin D precursors has been developed.Allylic oxidation of 3,5-cyclovitamin D derivatives, readily obtained from the buffered solvolysis of vitamin D tosylates, with selenium dioxide yields 1α-hydroxylated 3,5-cyclovitamin D compounds which are smoothly converted to the desired 1α-hydroxyvitamin D derivatives by acid-catalyzed cycloreversion.Application of this scheme to vitamin D3 (1a), 25-hydroxyvitamin D3 (1b), and vitamin D2 (1c) affords the 1α-hydroxy products in ca.20 percent overall yield.
- Paaren, Herbert E.,DeLuca, Hector F.,Schnoes, Heinrich K.
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p. 3253 - 3258
(2007/10/02)
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