CAS: 39552-01-7; 1-[7-[2-Hydroxy-3-(Propan-2-Ylamino)Propoxy]-1-Benzofuran-2-Yl]Ethanone

该化合物是一种主要用于治疗青光眼和眼部高血压的非选择性乙型肾上腺对抗物,通过抑制水幽默生产减少内部压力发挥作用.Befunolol的化学结构包括一个苯球类和二体膜,有助于其药理活动.其特点是能够穿透角膜屏障,从而增强其眼科应用的功效.Befunolol在进行专题时表现出相对较低的系统性吸收,最大限度地减少通常与乙型阻塞机有关的系统性副作用.此外,它具有抗氧化性特性,可能给眼部健康带来额外好处.该物质通常配成眼滴,并因其相对有利的安全性特征而闻名,尽管其潜在的副作用可包括局部刺激或过敏反应.与任何药物一样,必须在保健专业人员的指导下使用Befunolol,以确保适当的剂量和监测不良作用.

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      📜2-Phenyl-3-Isopropyl-5-(2-Acetyl-7-Benzofuranoxymethyl)Oxazolidine置于盐酸,Sodium Hydroxide体系中,化学反应生成 苯呋洛尔
      参考文献:Pharmaceutical Composition Containing Benzofuran Derivative
      标题:Pharmaceutical Composition Containing Benzofuran Derivative
      摘要:一种含有苯并呋喃衍生物作为主要活性成分的药物组合物,其化学式为:##str1## 其中a为--Cor',##str2## 或乙基基团;当a为--Cor'时,B为氢原子,##str3## 或在苯并呋喃核的3或4位处取代的--Cor",当a为乙基时;r为具有1至5个碳原子的烷基基团;r'为具有1至4个碳原子的烷基基团,具有1至3个碳原子的烷氧基或苯基;r"为具有1至4个碳原子的烷基基团,苯基或苯基烷基,其中烷基部分具有1至2个碳原子;取代的丙氧基基团位于苯并呋喃核的3,4,5,6或7位;或其在与药学上可接受的载体混合物中的药学上可接受的酸盐.该药物组合物具有卓越的β-肾上腺素受体阻滞活性和局部麻醉活性,适用于预防和治疗心脏疾病,高血压和甲状腺功能亢进症.

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      专利信息


      专利号:US-9353057-B2
      优先权日:2003-12-30
      标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
      发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
      权利人:XENOPORT INC
      摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

      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-2008287407-A1
      优先权日:2003-12-10
      标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
      发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
      权利人:NITROMED INC
      摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

      专利号:US-2015158809-A9
      优先权日:2013-02-26
      标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
      发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
      权利人:XENOPORT INC
      摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

      专利号:US-2008214827-A1
      优先权日:2004-02-03
      标 题:Synthesis of Cyanoimino-Benzoimidazoles
      发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
      权利人:EURO CELTIQUE SA
      摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

      专利号:WO-2009094569-A2
      优先权日:2008-01-25
      标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

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      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Koike K, Horinouchi T, Takayanagi I. Comparison of interactions of R(+)- and S(-)-isomers of beta-adrenergic partial agonists, befunolol and carteolol, with high affinity site of beta-adrenoceptors in the microsomal fractions from guinea-pig ciliary body, right atria and trachea. Gen Pharmacol. 1994 Nov;25(7):1477-81. German. German. German.
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