CAS: 124750-92-1; Losartan Carboxylic Acid

该化合物是用于抗血压药物的Losartan II 血管受体抗体抗体合成的关键中间体,这种碳本体酸衍生物的特点是纯度和稳定性高,适合制药生产过程,其结构特性确保下游化学转化的精确反应,有助于高效和一致的......

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CAS号124750-99-8 氯沙坦钾 | CAS号114798-26-4 氯沙坦 | CAS号1070174-98-9 2-butyl-4-chlor... | CAS号2387-23-7 N,N’-二环己基脲 | CAS号1070174-99-0 2-butyl-4-chlor... | CAS号947331-10-4 N-三苯甲基氯沙坦羧酸

合成工艺路线路线简述

    📜Losartan Potassium置于吡啶,Potassium Permanganate,四丁基氯化铵,盐酸体系中,用 水,丙酮 用作溶剂,化学反应 1.0H,以72%的收率获得氯沙坦
    参考文献:Preparation Of Losartan 5-Carboxylic Acid And Use Thereof
    标题:Preparation Of Losartan 5-Carboxylic Acid And Use Thereof
    摘要:一种合成洛卡特普5-羧酸(exp-3174)的方法.

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    专利信息


    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-2008090885-A1
    优先权日:2006-10-12
    标题:Preparation of losartan 5-carboxylic acid and use thereof
    发明人:CHEN LIQIN; LI JIAN; SHEN YINGZHONG
    权利人:CHEN LIQIN; LI JIAN; SHEN YINGZHONG
    摘要:A method for synthesis of losartan 5-carboxylic acid (EXP-3174).

    专利号:US-2006111369-A1
    优先权日:2004-11-10
    标 题:Synthesis, characterization and biological action of optically active isomers of floxacins
    发明人:SOMBERG JOHN C; RANADE VASANT V
    权利人:SOMBERG JOHN C; RANADE VASANT V
    摘要:Disclosed herein is the method for synthesis and separation of enantiospecific isomers of floxacins. These isomers can be used to study the antibacterial action, as well as cardiac effects, such as arrhythmogenic activity, QT internal prolongation and dispersion, and Ikr inhibition in humans. A method for the identification of chiral isolates of the floxacins that are devoid or possess less QT prolonging action and thus cause less arthropathy especially of the Torsades de pointes variety. Also disclosed are methods for assaying these isomeric compounds present in the biological fluids.

    专利号:US-6316487-B1
    优先权日:1993-06-16
    标 题:Compounds for treatment of cardiac arrhythmia synthesis, and methods of use
    发明人:DRUZGALA PASCAL; MILNER PETER G
    权利人:ARYX THERAPEUTICS
    摘要:The subject invention pertains to novel compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. The new compounds can have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The product can also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.

    专利号:US-2006074032-A1
    优先权日:2000-11-29
    标题 :Synthesis and separation of optically active isomers of erythromycin and their biological actions
    发明人:SOMBERG JOHN; RANADE VASANT
    权利人:ACADEMIC PHARM INC
    摘要:The present invention provides methods for purifying and using optically active isomers of erythromycin as well as compositions comprising such optically active isomers. Such optically active isomers having desired actions as an antibiotic substantially separable from undesirable effects on GI motility and the cardiac potassium channels such that the cardiac action potential is not prolonged and the QT interval on the surface EKG (electrocardiogram) is not increased, such that the erythromycin can be useful for more effective therapy of systemic infections. Also disclosed are methods for assaying the levels of such isomers present in the biological fluids.

    专利号:US-6869972-B2
    优先权日:2001-12-10
    标题 :Compounds for treatment of cardiac arrhythmia, synthesis, and methods of use
    发明人:DRUZGALA PASCAL
    权利人:ARYX THERAPEUTICS
    摘要:The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.

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    主要参考文献


    1: Choi JS, Choi JS, Choi DH. Effects of licochalcon A on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats. Pharmazie. 2013 Nov;68(11):882-8. doi: 10.1159/000328773. Epub 2011 Jun 25. doi: 10.1038/aps.2011.32. Epub 2011 Jun 13.
    4: Choi DH, Li C, Choi JS. Effects of myricetin, an antioxidant, on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats: possible role of cytochrome P450 3A4, cytochrome P450 2C9 and P-glycoprotein inhibition by myricetin. J Pharm Pharmacol. 2010 Jul;62(7):908-14. doi: 10.1211/jpp.62.07.0012. Epub 2006 Nov 21.
    7: Iwasa T, Takano T, Hara K, Kamei T. Method for the simultaneous determination of losartan and its major metabolite, EXP-3174, in human plasma by liquid chromatography-electrospray ionization tandem mass spectrometry. J Chromatogr B Biomed Sci Appl. 1999 Nov 12;734(2):325-30.

    合成参考文献


    参考文献:10.1111/j.1365-2710.2011.01279.x
    摘要:Yang L, Guo T, Xia DY, Zhao LS. Pharmacokinetics of losartan and its active carboxylic acid metabolite E-3174 in five ethnic populations of China. J Clin Pharm Ther. 2012 Apr;37(2):226–31. doi: 10.1111/j.1365-2710.2011.01279.x.
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