CAS: 162011-90-7; 4-(4-(Methylsulfonyl)Phenyl)-3-Phenylfuran-2(5H)-One

该化合物是一种非类固醇抗炎药物,属于选择性环氧氧素-2(COX-2)抑制剂,主要用于治疗骨髓炎,风湿素性关节炎和急性疼痛.Rofecexib通过有选择地抑制在发炎过程中起关键作用的COX-2酶来减少疼痛和炎症,从而减少疼痛和炎症,与抑制COX-1和COX-2的传统非固态消毒剂相比,其胃肠道副作用可能减少.该物质的特点是化学配方,其中包括一个磺酰胺组,有助于其药性特性.然而,Rofecoxib由于担心与其长期使用相关的心血管风险而于2004年退出市场.其药理学表明,它被很好地吸收并具有长期的半衰期,允许一次性服用.尽管其在疼痛管理方面的效率很高,但安全性特征导致对药物发展与治疗行动的潜在平衡.

结构式图片

欧盟法规

C&L通报

上下游产品

CAS号103-82-2 苯乙酸 | CAS号50413-24-6 4-甲砜基-α-溴代苯乙酮 | CAS号162012-30-8 3-(4-methylsulf... | CAS号201737-94-2 [2-(4-methylsul... | CAS号105-36-2 溴乙酸乙酯 | CAS号487047-31-4 3-chloro-4-(4'-... | CAS号98-80-6 苯硼酸 | CAS号7732-18-5 水 | CAS号121-44-8 三乙胺 | CAS号38654-91-0 2-(diethoxyphos... | CAS号185147-17-5 5-Hydroxy Vioxx | CAS号179174-76-6 2-(4-methylsulf...

合成工艺路线路线简述

  • 合成目标产物 Rofecoxib 主要起始原料 Phenylacetic Acid And 2-Bromo-1-[4-(Methylsulfonyl)Phenyl]-1-Ethanone
  • (文献来源)合成步骤主要原料 Phenylacetic Acid 和 2-Bromo-1-[4-(Methylsulfonyl)Phenyl]-1-Ethanone
2-(4-Methanesulfonylphenyl)-2-Oxoethyl 2-(Diethoxyphosphoryl)-2-Phenylacetate置于三乙胺体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 2.0H,以95%的收率获得罗非昔布
参考文献:3,4-二芳基取代2(5H)-呋喃酮的一锅法合成及其商业应用
标题:3,4-二芳基取代2(5H)-呋喃酮的一锅法合成及其商业应用
摘要:摘要 建立了3,4-二芳基取代的2(5H)-呋喃酮的一锅法合成方法,并通过完成罗非昔布的全合成,在温和的反应条件下,以非常好的收率和纯度证明了其商业应用.图形概要
Doi:10.1080/00397911.2011.577923

海关参考信息

专利信息


专利号:US-7692019-B2
优先权日:2000-12-04
标 题:Methods for the stereoselective synthesis of substituted piperidines
发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HEFFERNAN MICHELE L R; HOEMANN MICHAEL Z; KESSLER DONALD W; SHAO LIMING; WU XINHE; XIE ROGER L
权利人:SEPRACOR INC
摘要:One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-2003083352-A1
优先权日:2000-07-31
标 题 :Synthesis of imidazole intermediates
发明人:HELAL CHRISTOPHER J
权利人:PFIZER
摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-12264143-B2
优先权日:2020-12-17
标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use
发明人:SAMMIS GLENN M; ROGGEN MARKUS
权利人:NALU BIO INC
摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.

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
江苏省金坛市兢业医化技术研究所
⚠️ 未注册 · 未认证企业
⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
数据来源于公开网络搜索,平台未作核实,请自行辨别。
🏢敬请 企业认领
🏬开设公司展台
📢获取免费会员权益
🎖️点亮专属注册企业标签
📇展现公司完整信息 样本查看立即注册认领 →
网址: http://www.jy-chem.com
电话: 0519-82765788 82765761👤
📞江苏省金坛市兢业医化技术研究所 ⚠️参考联系方式

销售电话:0519-82765788 82765761
邮箱:yeyin@depeichem.com
🆔 联系时候可告知是从"百琢研"平台获取的信息.
⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

⚠️ 未注册 · 未认证企业
注册入口 备注: 📌 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别 ✉️ 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
第 1 / 1 页
现货

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献


1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Rofecoxib. 2020 Mar 20. 1(5):1053-66. doi: 10.1517/14656566.1.5.1053. VIGOR Study Group. Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. VIGOR Study Group. N Engl J Med. 2000 Nov 23;343(21):1520-8, 2 p following 1528. doi: 10.1056/NEJM200011233432103. 58(3):499-505; discussion 506-7. doi: 10.2165/00003495-199958030-00016. 2005(1):CD005115. doi: 10.1002/14651858.CD005115.
6: Matheson AJ, Figgitt DP. Rofecoxib: a review of its use in the management of osteoarthritis, acute pain and rheumatoid arthritis. Drugs. 2001;61(6):833-65. doi: 10.2165/00003495-200161060-00019. 55(7):859-94. doi: 10.1211/0022357021387. 5(1):55-61. doi: 10.1586/14737175.5.1.55. 23(9):1323-38. doi: 10.1016/s0149-2918(01)80112-0. 2005(1):CD003685. doi: 10.1002/14651858.CD003685.pub2.
11: Goy J, Paikin J, Crowther M. Rofecoxib does not appear to increase the risk of venous thromboembolism: a systematic review of the literature. Thromb Res. 2014 Nov;134(5):997-1003. doi: 10.1016/j.thromres.2014.08.030. Epub 2014 Sep 16. 4(3):491-9. doi: 10.1517/14740338.4.3.491. (2):CD003685. doi: 10.1002/14651858.CD003685. Update in: Cochrane Database Syst Rev. 2002;(3):CD003685. doi: 10.1002/14651858.CD003685. (3):CD003685. doi: 10.1002/14651858.CD003685. Update in: Cochrane Database Syst Rev. 2005 Jan 25;(1):CD003685. doi: 10.1002/14651858.CD003685.pub2. 2009(4):CD004604. doi: 10.1002/14651858.CD004604.pub3.

合成参考文献


参考文献:10.1007/bf03327445
摘要:Panza F, Solfrizzi V, Frisardi V, Imbimbo BP, Capurso C, D’Introno A, Colacicco AM, Seripa D, Vendemiale G, Capurso A, Pilotto A. Beyond the neurotransmitter-focused approach in treating Alzheimer’s Disease: drugs targeting β-amyloid and tau protein. Aging Clinical and Experimental Research. 2009 Dec;21(6):386–406. doi: 10.1007/bf03327445.
参考文献:10.18632/aging.100021
摘要:Choi SH, Bosetti F. Cyclooxygenase-1 null mice show reduced neuroinflammation in response to beta-amyloid. Aging (Albany NY). 2009 Feb 11;1(2):234–44.
参考文献:10.18632/aging.100039
摘要:Candelario-Jalil E. A role for cyclooxygenase-1 in beta-amyloid-induced neuroinflammation. Aging (Albany NY). 2009 Apr 13;1(4):350–3.
参考文献:10.1007/s00228-010-0789-2
摘要:Gudbjornsson B, Thorsteinsson SB, Sigvaldason H, Einarsdottir R, Johannsson M, Zoega H, Halldorsson M, Thorgeirsson G. Rofecoxib, but not celecoxib, increases the risk of thromboembolic cardiovascular events in young adults—a nationwide registry-based study. European Journal of Clinical Pharmacology. 2010 Feb 16;66(6):619–25. doi: 10.1007/s00228-010-0789-2.
参考文献:10.1016/j.bcp.2011.06.035
摘要:Imanishi J, Morita Y, Yoshimi E, Kuroda K, Masunaga T, Yamagami K, Kuno M, Hamachi E, Aoki S, Takahashi F, Nakamura K, Miyata S, Ohkubo Y, Mutoh S. Pharmacological profile of FK881(ASP6537), a novel potent and selective cyclooxygenase-1 inhibitor. Biochem Pharmacol. 2011 Oct 01;82(7):746–54. doi: 10.1016/j.bcp.2011.06.035.
📝 需求与反馈
尽可能描述清楚需求与问题信息
×

通知