CAS: 2438-72-4; 2-(4-Butoxyphenyl)-N-Hydroxyacetamide

该化合物是一种主要用于其止痛剂和抗炎特性的非类固醇抗炎药物,其特点是它能够抑制作为发炎和疼痛信号化合物的异丙菊酯的合成;Bufexamac经常用于治疗各种皮肤病,包括皮肤炎和乳房炎的时装配,因为其局部作用和相对于口服非甲状腺炎的系统性副作用减少;该物质通常以白色的形式呈现为非白晶状粉,有机溶剂中含有中等溶解性,水溶性有限;其行动机制包括抑制环氧酶酶,导致煽动性调味器的生产减少;尽管一般情况下,布非丁基氨酸可能会在一些人中造成皮肤刺激或过敏反应;与任何药物一样,必须在适当的医疗指导下使用二氟二酸盐,以确保安全和功效.

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ECHA物质C&L通报REACH预注册

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CAS号4547-57-3 4-丁氧基苯乙酸 | CAS号7803-49-8 羟胺

合成工艺路线路线简述

  • 合成目标产物 Bufexamac 主要起始原料 4-N-Butoxyphenylacetic Acid And Hydroxylamine
  • (文献来源)合成步骤主要原料 4-N-Butoxyphenylacetic Acid 和 Hydroxylamine
📜2-(4-Butoxyphenyl)-N-((Tetrahydro-2H-Pyran-2-yl)Oxy)Acetamide置于palladium 10% On Activated Carbon,氢气体系中,用 甲醇 用作溶剂,以75 %的收率获得丁苯羟酸
参考文献:阳光或 Uva 光介导的羧酸合成异羟肟酸
标题:阳光或 Uva 光介导的羧酸合成异羟肟酸
摘要:报道了阳光或 Uva 光介导的从羧酸和受保护的羟胺合成异羟肟酸的方法,其关键步骤是电荷转移复合物的形成.Di-Hrms 的机理研究为各种中间体的形成提供了实验证据.合成了两种异羟肟酸药物(伏立诺他和布非昔美).
Doi:10.1002/ejoc.202300046

海关参考信息

专利信息


专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

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-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:US-6281003-B1
优先权日:1996-05-20
标 题 :Enzymatic synthesis of optically active hydroxamic acids and their conversion to optically active primary amines by a lossen rearrangement
发明人:HIRRLINGER BEATE; STOLZ ANDREAS; KNACKMUSS HANS-JOACHIM
权利人:FRAUNHOFER GES FORSCHUNG
摘要:A method is described for the preparation of optically active hydroxamic acids of the general formula n wherein R 1 , R 2 and R 3 are different and are a cyclic or linear, aliphatic or aromatic, substituted or unsubstituted hydrocarbon radical which can optionally contain heteroatoms, said method being characterized in that a racemate of chiral amides, carboxylic acid esters or carboxylic acids of the general formula n wherein R 1 , R 2 and R 3 are as defined above and X is —NH 2 , —OR or —OH, R being any organic radical, n is reacted with hydroxylamine, NH 2 OH, in the presence of an acyltransferase, and the optically active hydroxamic acid (I) formed is then separated from the unconverted enantiomer of general formula (II). The resulting optically active hydroxamic acid can be converted to the corresponding optically active primary amines by a Lossen rearrangement.

专利号:US-9687428-B2
优先权日:2001-05-01
标题 :Hydrogel compositions for tooth whitening
发明人:SINGH PARMINDER; CLEARY GARY W; MUDUMBA SRI; FELDSTEIN MIKHAIL M; BAYRAMOV DANIR F
权利人:A V TOPCHIEV INST OF PETROCHEMICAL SYNTHESIS RUSSIAN ACAD OF SCIENCES; CORIUM INT INC; A V TOPCHIEV INST OF PETROCHEMICAL SYNTHESIS RUSSIAN ACAD OF SCIENCES
摘要:A composition is provided, wherein the composition comprises a water-swellable, water insoluble polymer, a blend of a hydrophilic polymer and a complementary oligomer capable of hydrogen bonding to the hydrophilic polymer, and a whitening agent, preferably a peroxide. The composition finds utility as a tooth whitening composition and is applied to the teeth in need of whitening, and then removed when the degree of whitening has been achieved. In certain embodiments, the composition is translucent. Methods for preparing and using the compositions are also disclosed.

专利号:AU-2022276509-A1
优先权日:2021-05-20
标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

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主要参考文献


1: Pan Y, Nixon R. Allergic contact dermatitis to topical preparations of bufexamac. Australas J Dermatol. 2012 Aug;53(3):207-10. doi: 10.1111/j.1440-0960.2012.00876.x. doi: 10.1016/j.jpba.2011.02.025. doi: 10.1097/DER.0b013e318260d774. doi: 10.1007/s00105-008-1656-2. German. doi: 10.1111/j.1346-8138.2011.01261.x. German. doi: 10.1111/j.1600-0536.2011.01883.x. doi: 10.1038/srep25298.
10: Trommer H, Plätzer M, Raith K, Wohlrab W, Podhaisky HP, Neubert RH. Examinations of the antioxidative properties of the topically administered drug bufexamac reveal new insights into its mechanism of action. J Pharm Pharmacol. 2003 Oct;55(10):1379-88. doi: 10.1111/j.1600-0536.2007.01271.x. German.

合成参考文献


摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
参考文献:10.1111/j.1346-8138.2004.tb00524.x
摘要:Arikawa J, Okabe S, Kaneko T. Allergic Contact Dermatitis with Spreading over Extensive Regions Due to Topical Use of 5% Bufexamac Ointment. The Journal of Dermatology. 2004 Feb;31(2):136–8. doi: 10.1111/j.1346-8138.2004.tb00524.x.
参考文献:10.1111/j.1600-0536.2007.01271.x
摘要:Belhadjali H, Ghannouchi N, Njim L, Mohamed M, Moussa A, Bayou F, Chakroun M, Zakhama A, Zili J. Acute generalized exanthematous pustulosis induced by bufexamac in an atopic girl. Contact Dermatitis. 2008 Apr;58(4):247–8. doi: 10.1111/j.1600-0536.2007.01271.x.
参考文献:10.1007/s00105-009-1812-3
摘要:Schauber J. [Topical therapy of perianal eczema]. Hautarzt. 2010 Jan;61(1):33–8. doi: 10.1007/s00105-009-1812-3.
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