215929-37-6Relevant academic research and scientific papers
Preparation method and application of calcipotriol impurity compound
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, (2020/10/21)
The invention discloses a preparation method of a calcipotriol impurity compound. (Z)-2-((3S, 5R)-3, 5-di(tert-butyldimethylsiloxy)-2-methylenecyclohexyl)ethyl diphenyl phosphine oxide is used as a raw material, and reacts with tetrabutylammonium fluoride in tetrahydrofuran; Swern oxidation, a reduction reaction and the like are carried out to obtain the calcipotriol impurity compound; and the compound is crystallized to obtain the (Z)-2-((3S, 5R)-3, 5-di(tert-butyldimethylsiloxy)-2-methylenecyclohexyl)ethyl diphenyl phosphine oxide. The preparation method has advantages of simple process, lowequipment requirement, and high calibration content of the obtained product, and provides guiding significance for the control of the drug quality.
Synthesis and evaluation of A-ring diastereomers of 1α,25-dihydroxy-22-oxavitamin D3 (OCT)
Hatakeyama, Susumi,Okano, Toshio,Maeyama, Junji,Esumi, Tomoyuki,Hiyamizu, Hiroko,Iwabuchi, Yoshiharu,Nakagawa, Kimie,Ozono, Keiichi,Kawase, Akira,Kubodera, Noboru
, p. 403 - 415 (2007/10/03)
A-ring diastereomers of 1α,25-dihydroxy-22-oxavitamin D3 (OCT) (2), 3-epi-1α,25-dihydroxy-22-oxavitamin D3 (3-epiOCT) (3) and 1,3-diepi-1α,25-dihydroxy-22-oxavitamin D3 (1,3-diepiOCT) (4) were synthesized by the convergent method. In vitro binding affinity for rat vitamin D binding protein and calf-thymus vitamin D receptor, differentiation-inducing activity on HL-60 cells, and transcriptional activity of 3-epiOCT (3) and 1,3-diepiOCT (4) were evaluated in comparison with OCT (2), 1-epi-1α,25-dihydroxy-22-oxavitamin D3 (1-epiOCT) (5) and 1α,25-dihydroxyvitamin D3 (1).
