CAS: 33564-31-7; Diflorasone Diacetate

该化合物是一种主要用于皮肤学应用的具有抗炎和免疫抑制特性的合成可溶性固醇类固醇,其特点是其强大的凝胶类活动,有助于减少炎症,缓解与各种皮肤状况有关的症状;该化合物通常是一种局部施药或奶油,可以局部处理诸如乙酰胺,皮质丝虫病和皮肤炎等情况;二氟芳二乙酸酯表现出对凝胶受体具有高度亲近性,导致其在调制免疫反应和抑制释放阻燃性调节器方面产生效力;其化学结构包括两个乙酸盐类,可增加其脂性,有利于改善皮肤的渗透和吸收;虽然该化合物在控制炎症方面是有效的,但对长期使用可能导致皮肤营养性或其他局部副作用提出告诫.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

6α-fluoro-9β,11β-epoxy-17α,21-dihydroxy-16β-methylpregna-1,4-diene-3,20-dione 17,21-diacetate 6α,9α-difluoro-11β,17α,21-trihydroxy-16β-methylpregn-4-ene-3,20-dione 17,21-diacetate 2,3-dicyano-5,6-dichloro-p-benzoquinone 6α-fluoro-16β-methyl-17α,21-diacetoxypregna-4,9(11)-diene-3,20-dione

合成工艺路线路线简述

    17α,21-Diacetoxy-6α-Fluoro-16β-Methyl-9β,11β-Oxidopregna-1,4-Dien-3,20-Dione 反应生成 醋酸双氟拉松
    参考文献:Process For Producing 6.Alpha.-Fluoro-.Delta..Sup.1,4-3-Keto Steroids
    标题:Process For Producing 6.Alpha.-Fluoro-.Delta..Sup.1,4-3-Keto Steroids
    摘要:本文介绍了一种转化6.Beta.-Fluoro-.Delta..Sup.1,4-3-Keto类固醇(Iv)为6.Alpha.-Fluoro-.Delta..Sup.1,4-3-Keto类固醇(Vi)的两种方法(一锅法和两锅法).这些方法允许在以前无法在6.Alpha.位置引入双键的.Delta..Sup.1,4-3-Keto类固醇中引入氟原子,直到6.Alpha.-Fluorine原子出现之后.6.Alpha.-Fluoro-.Delta..Sup.1,4-3-Keto类固醇(Vi)是制造药理活性类固醇的有用中间体.

    海关参考信息

    专利信息


    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:US-9315483-B2
    优先权日:2007-09-13
    标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
    发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

    专利号:WO-2022226312-A1
    优先权日:2021-04-22
    标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers
    发明人:KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES
    权利人:CLEAR CREEK BIO INC
    摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides

    专利号:US-9051302-B2
    优先权日:2008-01-15
    标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
    发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
    权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
    摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

    专利号:US-8802660-B2
    优先权日:2007-03-12
    标 题:De novo synthesis of glucocorticoids in the epidermis and its uses and applications
    发明人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H
    权利人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H; UNIV NEW YORK
    摘要:The present invention relates to methods and compositions that control, i.e., antagonize/inhibit or agonize/stimulate, de novo glucocorticoid production in the skin. Such methods and compositions can be used for the prevention and/or treatment of a variety of skin conditions, including inflammation, acute wounds, chronic non-healing wounds, keloid, fibrotic or hypertrophic scars, and epithelial-derived cancer.
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    主要参考文献


    1: Maccaroni E, Giovenzana GB, Palmisano G, Botta D, Volante P, Masciocchi N. Structures from powders: diflorasone diacetate. Steroids. 2009 Jan;74(1):102-11. doi: 10.1016/j.steroids.2008.09.014. Epub 2008 Oct 18. German. German. German. German. German. Italian. German. Italian.

    合成参考文献


    摘要:Drugs in Japan, -(487), 1990
    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
    摘要:Graham JS, Chilcott RP, Rice P, Milner SM, Hurst CG, Maliner BI. Wound healing of cutaneous sulfur mustard injuries: strategies for the development of improved therapies. J Burns Wounds. 2005 Jan 05;4():e1.
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