CAS: 613-92-3; N'-Hydroxybenzimidamide

该化合物是有机化合物,其特征是存在一个氨化物和氧化亚胺功能组,一般是白色到非白晶状的固体,分子结构是附于一个亚丁基组的苯环,有助于其反应和有机合成的潜在应用.本扎米多克斯因其与过渡金属形成协调综合体的能力而闻名,使其在各种化学反应中有用,包括涉及金属催化的化学反应.此外,它显示出可能与医药化学有关的特性,特别是制药方面的特性.该化合物在极地溶溶剂中溶解,可提高其在各种化学过程中的效用.安全数据表明,与许多有机化合物一样,它应该谨慎处理,因为如果被摄入或吸入,它可能会对健康造成危害.

结构式图片

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REACH注册ECHA物质C&L通报REACH预注册

上下游产品

ethyl N-hydroxybenzimidate (Z)-ethyl benzohydroximate benzohydroximic acid hydroxyamide benzamidine monohydr°Chloridepropionic acid3-(3-Phenyl)-1,2,4-oxadiazol-5-ylpropionic acid 2-(3-phenyl-1,2,4-oxadiazol-5-yl)benzoic acid N-ethoxycarbonyloxy-benzamidineN-ethoxycarbonyloxy-benzamidine 3-phenyl-4H-[1,2,4]oxadiazol-5-one

合成工艺路线路线简述

    苯甲腈置于吡啶,盐酸羟胺体系中,用 乙醇 作为反应溶剂,化学反应生成 苯甲酰胺肟
    参考文献:哌啶-螺恶二唑衍生物作为α7烟碱样受体拮抗剂的设计,合成和生物学活性.
    标题:哌啶-螺恶二唑衍生物作为α7烟碱样受体拮抗剂的设计,合成和生物学活性.
    摘要:α 已经提出在神经和免疫系统中表达的7种烟碱乙酰胆碱受体(nachrs)在炎症控制中起重要作用.然而,由于缺乏的拮抗剂工具特异性抑制α 7个的nachr阻碍通道作为治疗靶的验证.要发现的选择性α 7拮抗剂,我们开始了基于药效的虚拟筛选和鉴定的哌啶衍生物spirooxadiazole T761-0184充当α 7拮抗剂.随后在非洲爪蟾卵母细胞中合成了一系列新型哌啶-螺二恶唑衍生物,并使用两电极电压钳(tevc)分析对其进行了评估.两个系列的铅化合物均受抑制α7的ic 50值为3.3μm至13.7μm.化合物b10表现出α 7选择性超过其它α 4 β 2和α 3 β 4的nachr亚型.的结构-活性关系的分析(sar)提供了一种用于选择性的进一步发展了有价值的见解α 7的nachr拮抗剂.
    DOI:10.1016/j.Ejmech.2020.112774

    海关参考信息

    专利信息


    专利号:US-9944609-B2
    优先权日:2013-03-15
    标 题:Formation of N-protected bis-3,6-(4-aminobutyl)-2, 5-diketopiperazine through a cyclic alpha-N-protected amino ester
    发明人:FREEMAN JOHN J; PHANSTIEL OTTO; BAY WILLIAM ELLIOT; KRAFT KELLY SULLIVAN
    权利人:MANNKIND CORP
    摘要:A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic α-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.

    专利号:WO-2019182527-A1
    优先权日:2018-03-21
    标 题:Methyl jasmonate derivatives as possible drug candidates for use in treatment of cancer
    发明人:GUZEL MUSTAFA; OZDATLI SUKRAN; SAVLUG OZGECAN; SUCU BILGESU ONUR
    权利人:T C ISTANBUL MEDIPOL UNIV
    摘要:The present invention relates to the active methyl jasmonate analogues which are effective on the cancer disease and / or on the mechanisms that constitute the disease, the methods of synthesis of said analogs / derivatives and their use in the treatment of a variety of diseases, particularly for treatment of cancer and cancer-causing diseases.

    专利号:US-7071338-B2
    优先权日:2002-11-27
    标 题 :Process for the synthesis of bis-aryl diamidoxime compounds
    发明人:BOYKIN DAVID W; ANBAZHAGAN MARIAPPAN; TIDWELL RICHARD R
    权利人:UNIV GEORGIA STATE RES FOUND
    摘要:Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl] furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.

    专利号:US-6849650-B2
    优先权日:1998-02-27
    标 题:Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
    发明人:THORSETT EUGENE D; PORTER WARREN J; NISSEN JEFFREY S; LATIMER LEE H; AUDIA JAMES E; DROSTE JAMES
    权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI
    摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

    专利号:US-6399628-B1
    优先权日:1996-11-22
    标 题 :N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds
    发明人:AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; REEL JON K; THORSETT EUGENE D; WHITESITT CELIA A
    权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI
    摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

    专利号:EP-0951466-B1
    优先权日:1996-12-23
    标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
    发明人:WU JING; TUNG JAY S; THORSETT EUGENE D; PLEISS MICHAEL A; NISSEN JEFFREY S; NEITZ JEFFREY; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; DROSTE JAMES J; HENRY STEVEN S; MCDANIEL STACEY L; SCOTT WILLIAM L; STUCKY RUSSELL D
    权利人:ELAN PHARM INC; LILLY CO ELI
    摘要:Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
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    主要参考文献

    [参考文献]: A K Frhlich, Et Al. Metabolism Of Benzamidoxime (N-Hydroxyamidine) In Human Hepatocytes And Role Of Udp-Glucuronosyltransferases. Xenobiotica. 2005 Jan;35(1):17-25.
    [参考文献]: B Clement, Et Al. [参考文献]: Arch Pharm (Weinheim). 1989 Jul;322(7):431-5.
    [参考文献]: B Clement, Et Al. Biotransformation Of Benzamidine And Benzamidoxime In Vivo. Arch Pharm (Weinheim). 1993 Oct;326(10):807-12.
    [参考文献]: B Clement, Et Al. Characteristics Of The Microsomal N-Hydroxylation Of Benzamidine To Benzamidoxime. Xenobiotica. 1987 Jun;17(6):659-67.
    [参考文献]: B Clement, Et Al. Genotoxic Activities Of Benzamidine And Its N-Hydroxylated Metabolite Benzamidoxime In Salmonella Typhimurium And Mammalian Cells. J Cancer Res Clin Oncol. 1988;114(4):363-8.

    合成参考文献


    摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 197.
    摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 256.
    摘要:Campagne, J. M.; Leclerc, E., Science of Synthesis Knowledge Updates, (2020) 2, 165.
    参考文献:10.1007/bf00400749
    摘要:Frei E, Pool BL, Glatt HR, Gemperlein-Mertes I, Oesch F, Schlehofer JR, Schmezer P, Weber H, Wiessler M. Determination of DNA single strand breaks and selective DNA amplification by N-nitrodimethylamine and analogs, and estimation of the indicator cells' metabolic capacities. Journal of Cancer Research and Clinical Oncology. 1986 Apr;111(2):123–8. doi: 10.1007/bf00400749.
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