CAS: 54340-62-4; (+/-)-Bufuralol

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5-溴-Alpha-[[叔-丁基氨基]甲基]-7-乙基苯并呋喃-2-甲醇 5-Bromo-2-(2-Tert-Butylamino-1-Hydroxyethyl)-7-Ethylbenzofuran 85536-86-3
(R)-7-Ethyl-2-Oxiranyl-Benzofuran

合成工艺路线路线简述

    📜(R)-7-Ethyl-2-Oxiranyl-Benzofuran 以98% Ee; 54的收率获得产物丁呋洛尔
    参考文献:Tetrahedron: Asymmetr. 2014,25,1316-1322
    标题:Tetrahedron: Asymmetr. 2014,25,1316-1322

    海关参考信息

    专利信息


    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-7708989-B2
    优先权日:1999-10-29
    标题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency
    发明人:LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL
    权利人:NITROMED INC
    摘要:The invention provides methods of treating and/or preventing vascular diseases characterized by nitric oxide insufficiency by administering a therapeutically effective amount of at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated cholesterol reducer, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and optionally at least one compound used to treat cardiovascular diseases and/or at least one antioxidant, or a pharmaceutically acceptable salt thereof, and/or 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. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The 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 may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The vascular diseases characterized by nitric oxide insufficiency include a cardiovascular disease and a disease resulting from oxidative stress.

    专利号:US-7384976-B2
    优先权日:2001-05-02
    标 题:Nebivolol and its metabolites in combination with nitric oxide donors, compositions and methods of use
    发明人:GARVEY DAVID S
    权利人:NITROMED INC
    摘要:The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a 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 may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.

    专利号:US-11897827-B1
    优先权日:2022-11-22
    标 题 :Carbon isotope exchange mediated by vanadium complexes
    发明人:BUKHRYAKOV KONSTANTIN
    权利人:BUKHRYAKOV KONSTANTIN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
    摘要:The subject invention provides catalytical compounds/complexes, compositions comprising such compound/complex, synthesis of the compounds/complexes, and methods of using such compounds/complexes as catalysts in, for example, carbon isotope exchange (CIE) on target bioactive molecules. Methods that allow CIE directly on drug candidates are of great importance to chemistry, biology, and medicine. Especially valuable are catalytic procedures that rely on a limited collection of available labeled materials. The instant method comprises converting a methyl group to terminal â•?CH2 utilizing transfer dehydrogenation catalysts to enable V-based olefin metathesis, followed by a hydrogenation step. The one-pot strategy allows the formal methylation/demethylation sequence and can be applied to an assortment of alkyl-containing compounds.

    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.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Uehara S, Uno Y, Hagihira Y, Murayama N, Shimizu M, Inoue T, Sasaki E, Yamazaki H. Marmoset cytochrome P450 2D8 in livers and small intestines metabolizes typical human P450 2D6 substrates, metoprolol, bufuralol and dextromethorphan. Xenobiotica. 2015;45(9):766-72. doi: 10.3109/00498254.2015.1019595. Epub 2015 Jul 27. doi: 10.1111/bcpt.12478. Epub 2015 Sep 26.
    4: Johnston GD, Finch MB, Shanks RG. Peripheral vascular effects of bufuralol in hypertensive and normal subjects: a comparison with propranolol and pindolol. Eur J Clin Pharmacol. 1986;30(6):649-52.

    合成参考文献


    摘要:HANSCH,C ET AL. (1995)
    参考文献:10.1007/s002280050164
    摘要:Transon C, Lecoeur S, Leemann T, Beaune P, Dayer P. Interindividual variability in catalytic activity and immunoreactivity of three major human liver cytochrome P450 isozymes. European Journal of Clinical Pharmacology. 1996 Sep 02;51(1):79–85. doi: 10.1007/s002280050164.
    参考文献:10.1002/jps.10091
    摘要:Nakajima M, Tane K, Nakamura S, Shimada N, Yamazaki H, Yokoi T. Evaluation of Approach to Predict the Contribution of Multiple Cytochrome P450s in Drug Metabolism Using Relative Activity Factor: Effects of the Differences in Expression Levels of NADPH–Cytochrome P450 Reductase and Cytochrome b5 in the Expression System and the Differences in the Marker Activities. Journal of Pharmaceutical Sciences. 2002 Apr;91(4):952–63. doi: 10.1002/jps.10091.
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