CAS: 57333-96-7; (1R,3S,5Z)-5-[(2E)-2-[(1R,3As,7Ar)-1-[(2R,5R)-5-Hydroxy-6-Methylheptan-2-Yl]-7A-Methyl-2,3,3A,5,6,7-Hexahydro-1H-Inden-4-Ylidene]Ethylidene]-4-Methylidenecyclohexane-1,3-Diol

该化合物是维生素D3的合成衍生物,专门设计用于治疗psorplogic和其他皮肤病,主要作为维生素D模拟,促进调节皮肤细胞生长和差异.Tacalcitool对乳腺细胞产生了抗扩散作用,而乳腺细胞是皮皮皮动物的主要细胞类型,因此有助于减少与psorpicalpic有关的过量缩放和炎症.该化合物通常配制成一种奶油或膏剂,直接应用于受影响地区.其行动机制对维生素D受体具有约束力,导致与皮肤细胞变换有关的基因表达方式的调节.Tacalcitool一般发酵,副作用较低,尽管某些病人可能出现局部刺激.与任何药物一样,必须在保健专业人员的指导下使用tacalcitool,以确保治疗的安全和功效.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

(1S,3R,5E,7E)-1,3-二-[(叔-丁基二甲基硅烷基)氧基]-9,10-开环孕甾-5,7,10-三烯-20-甲醛 (5E,7E)-(1S,3R,20S)-1,3-Bis<<(1,1-Dimethylethyl)Dimethylsilyl>Oxy>-20-Methyl-9,10-Secopregna-5,7,10(19)-Trien-21-Al 112828-13-4

合成工艺路线路线简述

    De-A,B-(24R)-24-[(Methoxymethyl)Oxy]-Cholestan-8-One置于正丁基锂,氢氟酸,四丁基氟化铵体系中,用 四氢呋喃,水,乙腈 作为反应溶剂,化学反应 42.0H,反应生成 他卡西醇
    参考文献:修饰的julia烯化和α氨氧基化反应介导1α,24(R)-二羟基维生素d 3(他骨化醇)的收敛合成
    标题:修饰的julia烯化和α氨氧基化反应介导1α,24(R)-二羟基维生素d 3(他骨化醇)的收敛合成
    摘要:从廉价的和可商购的异戊醛和容易获得的inhoffen-Lythgoe二醇开始,已经实现了塔骨化醇的收敛合成.关键步骤包括脯氨酸催化的α氨氧基化和julia-Kocienski烯烃化.
    DOI:10.1016/j.Tetlet.2017.07.103

    海关参考信息

    专利信息


    专利号:WO-2025108575-A1
    优先权日:2023-11-21
    标 题:Methods of selective deprotection and synthesis of transhydrindane- skeleton-based compounds
    发明人:HUBER FLORIAN MAURITIUS ERASMUS
    权利人:ROCHE DIAGNOSTICS GMBH
    摘要:The present invention relates to methods of selectively deprotecting a transhydrindane-skeleton-based compound comprising at least two different silyl ether groups. The present invention further relates to methods of synthesizing a Vitamin D molecule and to Vitamin D molecules obtainable by such processes. Furthermore, the present invention relates to a compound according to formula (I) comprising two different silyl ether groups, its use in the synthesis of Vitamin D molecules and to methods of producing such a compound.

    专利号:US-6610866-B2
    优先权日:1996-12-06
    标 题 :Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds
    发明人:KINNEY WILLIAM A; JONES STEVEN; ZHANG XUEHAI; RAO MEENA N; BULLIARD MICHEL; MECKLER HAROLD; LEE NANCY
    权利人:MAGAININ PHARMA
    摘要:A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.

    专利号:EP-1389623-B1
    优先权日:1996-12-06
    标题 :Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin d analogs, and other compounds
    发明人:KINNEY WILLIAM A; JONES STEVEN; ZHANG XUEHAI; RAO MEENA N; BULLIARD MICHEL; MECKLER HAROLD; LEE NANCY
    权利人:OHR PHARMACEUTICAL INC

    专利号:JP-2009138000-A
    优先权日:1996-12-06
    标题 :Stereoselective synthesis of 24-hydroxylated compounds useful for the production of aminosterols, vitamin D analogs and other compounds

    专利号:CN-105439927-A
    优先权日:2014-09-29
    标题 :A kind of preparation method of enantioselective synthesis of tacalcitol

    专利号:WO-9824800-A2
    优先权日:1996-12-06
    标题 :Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin d analogs, and other compounds
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    主要参考文献


    1: Li C, Hu Y, Mu Z, Shi L, Sun X, Wang X, Wang Y, Li X. Comparison of various excimer laser (EL) combination therapies for vitiligo: a systematic review and network meta-analysis. J Dermatolog Treat. 2024 Dec;35(1):2302064. doi: 10.1080/09546634.2024.2302064. Epub 2024 Jan 17. 12(19):2387. doi: 10.3390/cells12192387.
    3: Chandy RJ, Dao DD, Rivis CC, Shan DM, Feldman SR. Noncorticosteroid Topical Therapies for the Treatment of Plaque Psoriasis: A Narrative Review. J Pharm Technol. 2023 Oct;39(5):247-255. doi: 10.1177/87551225231193057. Epub 2023 Aug 19.
    4: Thiel A, Hermanns C, Lauer AA, Reichrath J, Erhardt T, Hartmann T, Grimm MOW, Grimm HS. Vitamin D and Its Analogues: From Differences in Molecular Mechanisms to Potential Benefits of Adapted Use in the Treatment of Alzheimer's Disease. Nutrients. 2023 Mar 30;15(7):1684. doi: 10.3390/nu15071684.

    合成参考文献


    摘要:Yakuri to Chiryo. Pharmacology and Therapeutics., 17(4615), 1989
    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from
    参考文献:10.1007/s001050050918
    摘要:Freitag M, von Kobyletzki G, Pieck C, Altmeyer P. [Balneologic photochemotherapy of prurigo simplex subacuta]. Hautarzt. 1999 May;50(5):344–9. doi: 10.1007/s001050050918.
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