CAS: 74050-20-7; Hydrocortisone

该化合物是一种主要用于抗炎和免疫抑制特性的合成花生机,其特点是能够减少与各种皮肤状况(如乳胶和皮质丝虫病)有关的炎症并缓解其症状.该化合物是氢可溶液的衍生物,经过改良以增强其效力并减少系统性副作用.丙烯酸盐通常是一种专题准备,允许采用最低限度系统吸收的局部治疗.其行动机制包括抑制亲食性细胞素和抑制免疫反应,这有助于控制炎症,促进愈合.该物质一般都经过良好调控,但与所有花生类植物一样,可能具有潜在的副作用,特别是长期使用.在使用水分泌酮时,必须遵循医疗指导,以确保有效和安全的治疗.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

氢化可的松17-丙酸酯 Hydrocortisone 17-Propionate 65980-97-4
醋酸氢化可的松 Hydrocortisone Acetate 50-03-3
氢化可的松 Hydrocortisone 50-23-7

合成工艺路线路线简述

    氢化可的松置于吡啶,对甲苯磺酸,溶剂黄146体系中,用 甲醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 醋丙氢可的松
    参考文献:(多)阳离子 λ3-碘介导的仲醇氧化扩环
    标题:(多)阳离子 λ3-碘介导的仲醇氧化扩环
    摘要:在此,我们报告了一种通过仲醇与(聚)阳离子λ3-碘(n-Hvi)的亲电活化合成中环醚的简化方法.通过新型 2-Ome-吡啶连接的 N-Hvi 的独特反应性,在已建立的 α-消除途径上实现了 Co 键迁移的优异水平选择性.所得的 Hfip-缩醛很容易用一系列亲核试剂衍生化,为后续操作提供了多功能的功能手柄.还证明了这种方法在后期天然产物衍生化中的实用性,为面向多样性的合成和复杂性到多样性(ctd)工作提供了新工具.初期机理研究揭示了醇构象对反应途径的强烈影响,从而为该方法应用于复杂分子合成提供了预测能力.
    DOI:10.1002/ejoc.201800118

    海关参考信息

    专利信息


    专利号:WO-0112817-A1
    优先权日:1999-08-12
    标题:Evolution and use of enzymes for combinathorial and medicinal chemistry
    发明人:KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
    权利人:MAXYGEN INC; LIU LU; KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
    摘要:This invention provides libraries of recombinant derivatizing enzymes that are useful for biocatalytic synthesis of derivatives oforganic molecules, including lead compounds for pharmaceutical use. The recombinant derivatizing enzymes catalyze reactions such as modification or replacement of functional groups on the organicmolecules, or addition of chemical moieties onto preexisting functional groups. The use of recombinant enzyme libraries enables one to obtain enzymes that catalyze the formation of organic molecule derivatives that could not otherwise be made using only naturally occurring enzymes.

    专利号:US-8697730-B2
    优先权日:2007-10-26
    标题 :5-lipoxygenase activating protein (FLAP) inhibitor
    发明人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON
    权利人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON; PANMIRA PHARMACEUTICALS LLC
    摘要:Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

    专利号:US-12304912-B2
    优先权日:2020-07-28
    标 题 :Fused bicyclic RAF inhibitors and methods for use thereof
    发明人:BELFIELD ANDREW; JONES CLIFFORD DAVID; MARGATHE JEAN-FRANÇOIS; COLLETTO CHIARA
    权利人:JAZZ PHARMACEUTICALS IRELAND LTD
    摘要:The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.

    专利号:CA-3187393-A1
    优先权日:2020-07-28
    标题:Chiral synthesis of fused bicyclic raf inhibitors

    专利号:EP-4188923-A1
    优先权日:2020-07-28
    标题 :Chiral synthesis of fused bicyclic raf inhibitors

    专利号:WO-2022023450-A1
    优先权日:2020-07-28
    标题:Chiral synthesis of fused bicyclic raf inhibitors
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    主要参考文献


    1: Nuttall TJ, McEwan NA, Bensignor E, Cornegliani L, Löwenstein C, Rème CA. Comparable efficacy of a topical 0.0584% hydrocortisone aceponate spray and oral ciclosporin in treating canine atopic dermatitis. Vet Dermatol. 2012 Feb;23(1):4-10, e1-2. doi: 10.1111/j.1365-3164.2011.00992.x. Epub 2011 Jul 1. doi: 10.1111/j.1365-3164.2011.00993.x. Epub 2011 Jul 1.
    4: Wohlrab J, Beck GM, Neubert RH, Sischka U, Kreft B. Hydrocortisone aceponate activity and benefit/risk ratio in relation to reference topical glucocorticoids. Skin Pharmacol Physiol. 2010;23(4):177-82. doi: 10.1159/000288164. Epub 2010 Feb 25. doi: 10.1111/j.1748-5827.2009.00776.x. doi: 10.1111/j.1751-0813.2009.00447.x. doi: 10.4103/0378-6323.69093. doi: 10.1111/j.1365-3164.2009.00777.x. doi: 10.1111/j.1365-3164.2009.00756.x. Epub 2009 Apr 3. German. doi: 10.1111/vde.12285. Epub 2016 Jan 25. doi: 10.1111/j.1365-3164.2009.00782.x. doi: 10.1111/vde.12306. Epub 2016 Apr 24. doi: 10.14202/vetworld.2016.882-887. Epub 2016 Aug 22.
    18: Fujimura M, Ishimaru H. Influence of a Diester Glucocorticoid Spray on the Cortisol Level and the CCR4(+) CD4(+) Lymphocytes in Dogs with Atopic Dermatitis: Open Study. J Vet Med. 2014;2014:492735. doi: 10.1155/2014/492735. Epub 2014 Sep 21. Erratum in: J Vet Med. 2016;2016:6510347.

    合成参考文献


    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
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