CAS: 78-41-1; Triparanol

该化合物是属于胆固醇合成抑制剂类别的有机化合物,主要因其作为低胆固醇剂的作用而得到承认,这意味着它被用于降低体内胆固醇水平.Triparanol通过抑制酶7-de-氢胆固醇还原酶的功能,从而干扰胆固醇的生物合成.该化合物是白到白的晶状固体,在水中溶解,但在有机溶剂中可溶解.其分子式为C27H45NO,其分子重量相对较高.Triparanol历来用于治疗超胆固醇;然而,由于副作用和更有效的胆固醇低效药物的开发,其临床使用已经减少.此外,它也与某些不利影响有关,包括白内酯形成,导致其从许多地区市场退出.作为化学物质,它对于处理三氯酚的安全性协议十分重要.

结构式图片

欧盟法规

ECHA物质ECHA物质化妆品禁用物质清单C&L通报REACH预注册

合成工艺路线路线简述

    📜(4-(Dimethylamino)Phenyl)(P-Tolyl)Methanone置于potassium Tert-Butylate体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 4.17H,反应生成 曲帕拉醇
    参考文献:从苯胺到芳醚:一种温和条件下的简便,高效且多功能的合成方法
    标题:从苯胺到芳醚:一种温和条件下的简便,高效且多功能的合成方法
    摘要:我们通过醇/酚(roh)与芳基铵盐(arnme反应开发了用于芳基醚的合成的简单且直接的方法3 +),它很容易从苯胺制备(arnr' 2,R'= H或me) .该反应在室温下顺利地且快速地进行(在几个小时内)在市售的碱,例如ko的存在吨卜或khmds,并具有相对于二者roh和arnr'宽的底物范围2.它具有可扩展性,并且与各种功能组兼容.
    DOI:10.1002/anie.201712618

    海关参考信息

    专利信息


    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-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-2006009642-A1
    优先权日:2001-10-12
    标题 :Methods for the synthesis of substituted purines
    发明人:DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G
    权利人:IRM LLC
    摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.

    专利号:US-6949644-B2
    优先权日:2001-10-12
    标题 :Methods for the synthesis of substituted purines
    发明人:DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G
    权利人:SCRIPPS RESEARCH INST
    摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines. In one aspect, the present invention provides a method of preparing a 2,6,9-substituded purine compounds of Formula I: n n nthe method comprising:n a) oxidizing a resin-bound compound of Formula II: n n to provide a resin-bound compound of Formula III: n n b) reacting the compound of Formula III with an amine of Formula IVn nNR 3 R 4   IV,n nto provide a resin-bound compound of Formula V n n c) cleaving the resin-bound compound of Formula V from the resin to provide the substituted purine compounds of Formula I.

    专利号:US-9220714-B2
    优先权日:2006-03-16
    标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
    发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
    权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
    摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

    专利号:US-2015352230-A1
    优先权日:2013-01-11
    标 题:Synthesis and isolation of dendrimer based imaging systems
    发明人:MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK
    权利人:UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).

    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: Officioso A, Manna C, Alzoubi K, Lang F. Triggering of Erythrocyte Death by Triparanol. Toxins (Basel). 2015 Aug 24;7(8):3359-71. doi: 10.3390/toxins7083359.
    2: Bi X, Han X, Zhang F, He M, Zhang Y, Zhi XY, Zhao H. Triparanol suppresses human tumor growth in vitro and in vivo. Biochem Biophys Res Commun. 2012 Aug 31;425(3):613-8. doi: 10.1016/j.bbrc.2012.07.136. Epub 2012 Aug 1. Erratum in: Biochem Biophys Res Commun. 2012 Nov 2;427(4):808. doi: 10.1371/journal.pone.0058833. Epub 2013 Mar 15.
    7: Rhoads DE, Kaneshiro ES. Fatty acid metabolism in Paramecium. Oleic acid metabolism and inhibition of polyunsaturated fatty acid synthesis by triparanol. Biochim Biophys Acta. 1984 Aug 15;795(1):20-9. Italian.

    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
    参考文献:10.1007/s00253-002-0932-9
    摘要:Manzoni M, Rollini M. Biosynthesis and biotechnological production of statins by filamentous fungi and application of these cholesterol-lowering drugs. Applied Microbiology and Biotechnology. 2002 Feb 14;58(5):555–64. doi: 10.1007/s00253-002-0932-9.
    摘要:Otto HF. [Changes of the submucous plexus (Meissner) and smooth muscles in experimental inhibition of cholesterol biosynthesis by triparanol. Ultramorphologic findings in the rat duodenum]. Zentralbl Allg Pathol. 1972;115(3):445–52.
    摘要:Otto HF. [Changes of the small intestine epithelium in experimental inhibition of cholesterol biosynthesis through triparanol. Light and electron microscopy findings]. Zentralbl Allg Pathol. 1972;115(5):588–99.
    摘要:Ono T. [Intermediary metabolic sterols in animal tissues]. Seikagaku. 1966 Jun;38(6):283–90.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知