CAS: 86541-78-8; (S)-2-(((S)-1-(Carboxymethyl)-2-Oxo-2,3,4,5-Tetrahydro-1H-Benzo[b]Azepin-3-yl)Amino)-4-Phenylbutanoic Acid

该化合物是一种抗血管素抗酶素抗酶素抗酶素(ACE)抑制剂,主要用于治疗高血压和心脏衰竭,是作为药物的抗甲酸丙酯的一种活性代谢物,是一种抗生素I(Angiotensin I)转化为血管素II(一种强大的血管抑制剂,从而导致血管炎和血压下降).Benazeprilat的化学结构包括一个对它的活动至关重要的碳毒剂组,其特点是它能够与ACE酶结合.它通常通过口服,具有相对长的半衰期,允许每天一次服用.Benazeprilat一般都受到抑制,但像其他抗生素抑制剂一样,它可能在某些病人中造成诸如咳嗽,高血糖和血管血肿等副作用.它的红外科效应可能受到诸如肾功能等因素的影响,而这种作用又能够对某种人群进行有效的心血管控制.

结构式图片

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CAS号86541-77-7 盐酸贝那普利 | CAS号4424-80-0 1,3,4,5-四氢-2H-1... | CAS号86499-22-1 3,3-二氯-2,3,4,5-... | CAS号86499-23-2 α-氯代苯并己内酰胺 | CAS号86499-53-8 (3S)-3-amino-1-... | CAS号86499-52-7 (S)-3-Amino-2,3...

合成工艺路线路线简述

  • 86541-74-4 = 86541-78-8
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Methanol,Water
    标题:Synthesis And Biological Properties Of (Carboxyalkyl)Amino-Substituted Bicyclic Lactam Inhibitors Of Angiotensin Converting Enzyme
    作者:Watthey,Jeffrey W. H.; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:1985 卷标:28(10) 页码:1511-16]

    64920-29-2 + 86499-53-8 = 86541-78-8
    反应条件:1.1 Reagents: Sodium Cyanoborohydride Solvents: Acetic Acid,Methanol1.2 Reagents: Hydrochloric Acid2.1 Reagents: Sodium Hydroxide Solvents: Methanol,Water
    标题:Synthesis And Biological Properties Of (Carboxyalkyl)Amino-Substituted Bicyclic Lactam Inhibitors Of Angiotensin Converting Enzyme
    作者:Watthey,Jeffrey W. H.; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:1985 卷标:28(10) 页码:1511-16]

    86499-52-7 = 86541-78-8
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Methanol,Water2.1 Reagents: Sodium Cyanoborohydride Solvents: Acetic Acid,Methanol2.2 Reagents: Hydrochloric Acid3.1 Reagents: Sodium Hydroxide Solvents: Methanol,Water
    标题:Synthesis And Biological Properties Of (Carboxyalkyl)Amino-Substituted Bicyclic Lactam Inhibitors Of Angiotensin Converting Enzyme
    作者:Watthey,Jeffrey W. H.; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:1985 卷标:28(10) 页码:1511-16
📜盐酸贝那普利置于sodium Hydroxide体系中,化学反应 0.5H,反应生成 贝那普利拉
参考文献:开发和验证不同方法处理零级和一级光谱测定部分重叠的混合物苯那普利和氨氯地平的比较研究
标题:开发和验证不同方法处理零级和一级光谱测定部分重叠的混合物苯那普利和氨氯地平的比较研究
摘要:已经开发了三种简单,选择性和准确的分光光度法,然后经过验证可用于散装散剂和药物剂型中的贝那普利(benz)和氨氯地平(aml)的分析.第一种方法是零阶吸收系数(af)和一阶光谱的幅度系数(pf),其中benz和aml均可从其在238 Nm处解析的零阶光谱或在253 Nm处的一阶光谱进行测量.第二种方法是针对零阶的常数乘法与恒定减法(cm-Cs)以及针对一阶光谱的连续导数减法-常数乘法(sds-Cm),其中benz和aml均可从其解析的零阶光谱中进行测量分别在240 Nm和238 Nm 或分别来自benazepril和amlodipine在214 Nm和253 Nm的一级光谱.第三种方法是新颖的常数乘积与导数零交叉(cm-Dzc)结合,这是一种在存在苯那普利主要降解产物贝那普利特(benzt)的情况下测定贝那普利和氨氯地平的稳定性指示测定方法.三种方法均按照ich指南进行了验证,贝那普利和氨氯地平的标准曲线在5-60μg/
DOI:10.1016/j.Saa.2016.03.047

海关参考信息

专利信息


专利号:US-8431712-B2
优先权日:2004-02-09
标 题 :Methods for the synthesis of pyridoxamine
发明人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT
权利人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT; NEPHROGENEX INC
摘要:The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): n nand salts thereof.n nThe invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.

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-7214799-B2
优先权日:2004-02-09
标题 :Methods for the synthesis of pyridoxamine

专利号:US-2007161678-A1
优先权日:2004-02-09
标题:Methods for the synthesis of pyridoxamine

专利号:US-2005272781-A1
优先权日:2004-02-09
标 题 :Methods for the synthesis of pyridoxamine

专利号:US-4410520-A
优先权日:1981-11-09
标题 :3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
发明人:WATTHEY JEFFREY W H
权利人:CIBA GEIGY CORP
摘要:Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzaz epin-2-ones and functional derivatives are angiotension converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.

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主要参考文献


1: Serrano-Rodríguez JM, Gómez-Díez M, Esgueva M, Castejón-Riber C, Mena-Bravo A, Priego-Capote F, Ayala N, Caballero JM, Muñoz A. Pharmacokinetic/pharmacodynamic modeling of benazepril and benazeprilat after administration of intravenous and oral doses of benazepril in healthy horses. Res Vet Sci. 2017 Mar 28;114:117-122. doi: 10.1016/j.rvsc.2017.03.016. [Epub ahead of print] doi: 10.1007/112_2015_27. Review. doi: 10.1111/jvp.12252. Epub 2015 Jul 30. doi: 10.1007/s11095-014-1587-9. Epub 2014 Dec 2. doi: 10.1016/j.jpba.2014.05.005. Epub 2014 May 13. Chinese. doi: 10.1186/1475-2840-12-169.
8: Kelers K, Devi JL, Anderson GA, Zahra P, Vine JH, Whittem T. Bioequivalence of a new liquid formulation of benazepril compared with the reference tablet product. Aust Vet J. 2013 Aug;91(8):312-9. doi: 10.1111/avj.12080. doi: 10.1016/j.chroma.2012.11.044. Epub 2012 Nov 27. doi: 10.1042/CS20120448.
11: Chen K, Zhang J, Liu S, Zhang D, Teng Y, Wei C, Wang B, Liu X, Yuan G, Zhang R, Zhao W, Guo R. Simultaneous determination of lercanidipine, benazepril and benazeprilat in plasma by LC-MS/MS and its application to a toxicokinetics study. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Jun 15;899:1-7. doi: 10.1016/j.jchromb.2012.04.014. Epub 2012 May 8. doi: 10.1111/j.1365-2885.2012.01406.x. Epub 2012 May 8. doi: 10.1586/erc.10.159. Review. doi: 10.1152/ajpheart.91493.2007. Epub 2008 Feb 22. Epub 2007 Aug 31. Epub 2007 Mar 31. Epub 2007 Jan 17. Epub 2006 Feb 28.

合成参考文献


参考文献:10.2165/00044011-199816060-00006
摘要:Aldigier JC, Meur YL, Brunel P. Protection of Renal Function with ACE Inhibitors: Experience with Benazepril. Clin Drug Investig. 1998;16(6):463–72. doi: 10.2165/00044011-199816060-00006.
参考文献:10.1016/j.jpba.2014.05.005
摘要:Rezk MR, Badr KA. Development, optimization and validation of a highly sensitive UPLC–ESI-MS/MS method for simultaneous quantification of amlodipine, benazeprile and benazeprilat in human plasma: Application to a bioequivalence study. Journal of Pharmaceutical and Biomedical Analysis. 2014 Sep;98():1–8. doi: 10.1016/j.jpba.2014.05.005.
参考文献:10.2165/00003088-199222050-00004
摘要:Burnier M, Biollaz J. Pharmacokinetic optimisation of angiotensin converting enzyme (ACE) inhibitor therapy. Clin Pharmacokinet. 1992 May;22(5):375–84. doi: 10.2165/00003088-199222050-00004.
参考文献:10.2165/00129784-200202040-00006
摘要:Wellington K, Goa KL. Valsartan: in chronic heart failure. Am J Cardiovasc Drugs. 2002;2(4):267–74; discussion 275. doi: 10.2165/00129784-200202040-00006.
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