CAS: 676129-92-3; Desvaleroyl Valsartan

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CAS号137862-53-4 缬沙坦

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    📜缬沙坦置于水,Sodium Hydroxide体系中,化学反应 24.0H,反应生成 N-[[2'(-(1H-四唑-5-基)[1,1'(-联苯]-4-基]甲基]-L-缬氨酸
    参考文献:Isolation And Characterization Of Novel Degradation Products Of Valsartan By NMR And High Resolution Mass Spectroscopy: Development And Validation Of Valsartan By Uplc
    标题:Isolation And Characterization Of Novel Degradation Products Of Valsartan By NMR And High Resolution Mass Spectroscopy: Development And Validation Of Valsartan By Uplc
    摘要:Valsartan被用于治疗高血压,心力衰竭和糖尿病肾病.它经过了酸性,碱性和过氧化物介导的氧化强制降解.强制降解是按照ich指南q1A(R2)-新药物物质和产品的稳定性测试进行的.在过氧化物介导的水解下,该药物是惰性的,碱性水解形成了两种降解物(dp-Val-1,Dp-Val-2),酸性水解形成了一种降解物(dp-Val-3).这些降解物最初是通过lc-Ms鉴定并通过质量介导纯化系统分离的.dp-Val-1和dp-Val-3已经报道,但它们的结构尚未通过2D NMR研究得到确认.dp-Val-2是一种新的降解物,其结构已通过高分辨率质谱和1D,2D NMR光谱的实质分析得到阐明.dp-Val-1由旋转异构体混合物组成,这个假设已通过可变温度NMR(vt-NMR)得到确认.开发并验证了一种稳定性指示rp-Uplc方法,用于测定valsartan Api药物的含量.在acquity Beh C-18 2.1x100Mm,1.7μm柱上验证了valsartan Uplc方法,运行时间缩短至6分钟,并按照监管指南在特异性,准确性,线性,精密度,检测限和定量限方面进行了验证.
    DOI:10.14233/ajchem.2020.22526

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    专利信息


    专利号:US-7728024-B2
    优先权日:2005-07-11
    标 题:Metal salts of 2′-(1H-Tetrazol-5yl)-1.1′-biphenyl-4-carboxaldehyde
    发明人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE
    权利人:NOVARTIS AG
    摘要:The invention relates to a method or process for the manufacture of blood pressure lowering agents, such as valsartan, novel intermediates as well as process steps in said synthesis. The method or process leads via the novel intermediate salts of the formula IA, n nor a tautomer thereof, wherein [kat] n+ is a cation and n is 1, 2, 3, 4, 5 or 6.

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    主要参考文献


    1: Monosilio S, Filomena D, Luongo F, Sannino M, Cimino S, Neccia M, Mariani MV, Birtolo LI, Benedetti G, Tonti G, Pedrizzetti G, Vizza CD, Maestrini V, Agati L. Cardiac and Vascular Remodeling After 6 Months of Therapy With Sacubitril/Valsartan: Mechanistic Insights From Advanced Echocardiographic Analysis. Front Cardiovasc Med. 2022 May 18;9:883769. doi: 10.3389/fcvm.2022.883769.
    2: Minotti G, Menna P, Camilli M, Salvatorelli E, Levi R. Beyond hypertension: Diastolic dysfunction associated with cancer treatment in the era of cardio- oncology. Adv Pharmacol. 2022;94:365-409. doi: 10.1016/bs.apha.2022.02.002. Epub 2022 Mar 30. 10(6):415-427. doi: 10.1016/j.jchf.2022.01.020. Epub 2022 Apr 6. 10(6):380-392. doi: 10.1016/j.jchf.2022.04.006.
    156:111303. doi: 10.1016/j.foodres.2022.111303. Epub 2022 May 7.

    合成参考文献


    参考文献:10.1016/j.jpba.2009.05.024
    摘要:Sampath A, Reddy AR, Yakambaram B, Thirupathi A, Prabhakar M, Reddy PP, Reddy VP. Identification and characterization of potential impurities of valsartan, AT1 receptor antagonist. Journal of Pharmaceutical and Biomedical Analysis. 2009 Oct;50(3):405–12. doi: 10.1016/j.jpba.2009.05.024.
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