CAS: 32222-06-3; (1R,3S,Z)-5-(2-((1R,3As,7Ar,E)-1-((R)-6-Hydroxy-6-Methylheptan-2-yl)-7A-Methyloctahydro-4H-Inden-4-Ylidene)Ethylidene)-4-Methylenecyclohexane-1,3-Diol

上下游产品

(1R,3aR,7aR)-1-{(1R)-1,5-dimethyl-5-[(trimethylsilyl)oxy]hexyl}-7a-methyl°Ctahydro-4H-inden-4-one [(2Z)-2-[(3S,5R)-3,5-bis(tert-butyldimethylsilanyloxy)-2-methylenecyclohexylidene]ethyl]diphenylphosphine oxide methyllithium 31α-Hydroxy-25-oxo-27-norvitamin D33[2H]-Pre-1,25-D3 31-Oxo-25-hydroxyprevitamin D3 (19)-triene-1,3,25-triol(1S),3(R)-9,10-sec°Cholesta-5(E),7(E),10(19)-triene-1,3,25-triol -9,10-sec°Cholesta-5(Z),7(E),10(19)-trien-25-ol(1S),3(R)-bis(tert-butyldimethylsilyl)oxy-9,10-sec°Cholesta-5(Z),7(E),10(19)-trien-25-ol

阿法骨化醇置于d-葡萄糖-6-磷酸,Bovine Adrenodoxin Reductase,Mouse 25-Hydroxyvitamin D3 1α-Hydroxylase,Mouse Adrenodoxin,水,还原型辅酶ii(Nadph)四钠盐,Glucose 6-Phosphate Dehydrogenase体系中,化学反应生成 骨化三醇
参考文献:小鼠25-羟基维生素d31α-羟化酶(cyp27B1)并入磷脂囊泡的底物的代谢
标题:小鼠25-羟基维生素d31α-羟化酶(cyp27B1)并入磷脂囊泡的底物的代谢
摘要:Cyp27B1催化25-羟基维生素d3的1α-羟基化为1α,25-二羟基维生素d3(维生素d3的激素活性形式).为了进一步表征小鼠cyp27B1,它在大肠杆菌中表达,纯化并在掺入磷脂囊泡的底物上测量了其活性,磷脂囊泡是内部线粒体膜的模型.囊泡中的25-羟基维生素d3和25-羟基维生素d2以相似的动力学经历1α-羟基化,催化速率常数(k Cat)分别为41和48 Mol / Min / Mol P450,而k M值为5.9和4.6 Mmol / Min Mol的磷脂分别.当膜中底物浓度大于k的4倍时,Cyp27B1显示出抑制作用m,与25-羟基维生素d2相比,使用25-羟基维生素d3更明显.由二油酰基磷脂酰胆碱和心磷脂制备的囊泡中的催化效率高于二肉豆蔻酰基磷脂酰胆碱囊泡.cyp27B1也催化与囊泡相关的24 R的1α-羟基化,25-二羟基维生素d3和20-羟基维生素d3以及1α-羟基维生素d
DOI:10.1016/j.Jsbmb.2010.02.022

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-4226770-A
优先权日:1978-02-10
标题:Synthesis of steroids
发明人：KAISER EMIL T
权利人:KAISER EMIL T
摘要:The synthesis of 1α,25-dihydroxycholesterol, 1α,25-dihydroxy-7-dehydrocholesterol and 1α,25-dihydroxycholecalciferol and other sterol derivatives from bile acids. Also the synthesis of 3,6-diketo steroids useful in the production of 1α,25-dihydroxycholesterol and other sterols which are biologically active or can be converted to biologically active sterols. The invention involves the sterols so produced and the processes by which they are prepared.

专利号:US-4163744-A
优先权日:1978-02-10
标 题:Synthesis of steroids
发明人：KAISER EMIL T
权利人:KAISER EMIL T
摘要:The synthesis of 1α,25-dihydroxycholesterol, 1α,25-dihydroxy-7-dehydrocholesterol and 1α,25-dihydroxycholecalciferol and other sterol derivatives from bile acids. Also the synthesis of 3,6-diketo steroids useful in the production of 1α,25-dihydroxycholesterol and other sterols which are biologically active or can be converted to biologically active sterols. The invention involves the sterols so produced and the processes by which they are prepared.

专利号:US-5292977-A
优先权日:1992-02-05
标题:Palladium catalyzed alkylative cyclization useful in synthesis of vitamin D and analogues
发明人：TROST BARRY M; DUMAS JACQUES
权利人:UNIV LELAND STANFORD JUNIOR
摘要:An alkylative cycloaddition method is provided that is particularly useful for the synthesis of many of the Vitamin D analogues with differing side chains. Thus, a preferred synthesis is of Vitamin D analogues having a side chain R 1 where a substantially geometrically pure first precursor having the structure ##STR1## and a second precursor are provided, the second precursor being a 1,7 enyne. These precursors are reacted in the presence of a palladium catalyst to form compounds having the structure ##STR2## where R 2 hydrogen, hydroxyl, lower alkoxy, fluorine, or a protecting group, and R 3 is hydrogen, hydroxyl, lower alkoxy, fluorine, or a protecting group.

专利号:US-6844461-B2
优先权日:2001-07-30
标 题:Synthesis of A-ring synthon of 19-NOR-1α,25-dihydroxyvitamin D3 from (D)-glucose
发明人：DELUCA HECTOR F; SHIMIZU MASATO; YAMADA SACHIKO
权利人:WISCONSIN ALUMNI RES FOUND
摘要:The present invention provides a method for the synthesis of an A-ring synthon phosphine oxide used in the preparation of 19-nor vitamin D compounds, and to novel synthetic intermediates formed during the synthesis. The new method prepares the phosphine oxide from (D)-glucose.

专利号:US-9994508-B2
优先权日:2012-12-11
标 题:Versatile and functionalised intermediates for the synthesis of vitamin D and novel vitamin D derivatives
发明人：LOPEZ PEREZ BORJA; SIGUEIRO PONTE RITA; MAESTRO SAAVEDRA MIGUEL A; MOURINO MOSQUERA ANTONIO
权利人:ENDOTHERM GMBH
摘要:Novel intermediates for the complete synthesis of vitamin D are provided that allow a great versatility of functional groups in the final vitamin derivatives. Vitamin derivatives that are epimeric in position 3 and vitamin derivatives with a wide range of functionalities in position 18, including compounds with isotopic labelling are provided.