CAS: 41292-65-3; 1H-Benzo[d]Imidazol-5-Ol

该化合物是一种七环有机化合物,其特点是一个苯并二氮卓核核心,在5号位置有氢氧基替代物,这种结构具有独特的反应性,使其成为制药和农用化学合成中有价值的中间体,其结合的芳香系统增强了稳定性,而氢氧气组则提供了一个可进一步发挥作用的多功能场所,如乙化或酯化.该复合体的硬脚手架在生物活性分子的设计中很有优势,特别是在发展酶抑制剂或受体调节器方面.具有高纯度,以确保研究和工业应用的一致性.建议,由于氧化的潜在敏感性,在惰性条件下进行适当的处理.

结构式图片

相似化合物

67021-83-4 4887-80-3 92335-78-9

欧盟法规

C&L通报

上下游产品

CAS号4887-80-3 5-甲氧基苯并咪唑 | CAS号610-81-1 3-硝基-4-氨基苯酚 | CAS号122-51-0 原甲酸三乙酯 | CAS号64-18-6 甲酸 | CAS号16133-49-6 5-甲氧基-2-硝基苯胺 | CAS号102-51-2 4-甲氧基邻苯二胺 | CAS号50591-21-4 1H-Benzimidazol... | CAS号124841-30-1 1H-苯并咪唑-5-醇,4-氯 | CAS号57050-67-6 (9ci)-4-[(二甲基氨基...

合成工艺路线路线简述

    5-甲氧基苯并咪唑置于氢溴酸体系中,用 水 作为反应溶剂,以51 %的收率获得产物1H-苯并咪唑-5-醇
    参考文献:开发用于脑肿瘤 Sigma-2 受体成像的高度特异性 18F 标记放射性配体
    标题:开发用于脑肿瘤 Sigma-2 受体成像的高度特异性 18F 标记放射性配体
    摘要:设计并合成了具有 6,7-二甲氧基-1,2,3,4-四氢异喹啉或 5,6-二甲氧基异吲哚啉药效团的新型配体,用于评估其与 Sigma-2 (σ 2) 受体的结构-活性关系,并开发了这些配体作为合适的 Pet 放射性配体.化合物1对 σ 2受体具有纳摩尔级亲和力(k I (σ 1) = 2.57 Nm),高亚型选择性(>2000 倍)以及对 40 种其他受体和转运蛋白的高选择性.制备的放射性配体[18 F] 1的放射化学产率为37-54%,放射化学纯度> 99%,摩尔活度为107-189 Gbq/μmol.小鼠中的生物分布和阻断研究以及大鼠中的[18 F] 1显微 Pet/ct 成像表明其与体内σ 2受体具有优异的结合特异性.u87Mg 胶质瘤异种移植模型中的 [18 F] 1显微 Pet/ct 成像显示出清晰的肿瘤可视化,具有高肿瘤摄取和肿瘤背景比.与 Cm398 (5 μmol/kg)
    DOI:10.1021/acs.Jmedchem.3C00735

    海关参考信息

    专利信息


    专利号:US-6262253-B1
    优先权日:1993-05-24
    标 题 :Vitamin B12 conjugates with gcsf, analogues thereof and pharmaceutical compositions
    发明人:RUSSELL-JONES GREGORY JOHN; WESTWOOD STEVEN WILLIAM
    权利人:BIOTECH AUSTRALIA PTY LTD
    摘要:The invention describes complexes between VB12 analogues and either GCSF or EPO that retain both significant affinity for intrinsic factor (IF) in the VB12 portion of the complex and significant bioactivity of the GCSF or EPO portion of the complex. The invention also concerns a process for the synthesis of these complexes. This is achieved at least in part, by using a spacer compound, which is linked covalantly between the VB12 portion and the GCSF or EPO. The complexes preferably have the formulawherein V is vitamin B12 or a vitamin B12 analogue, or derivative, bonded to X either through a carboxylate group pendant to the corrin nucleus of VB12 or through the central cobalt atom or to a functional group introduced onto the VB12 molecule, X is selected from: -NHNH-, -NH-, -O-, -S-, -SS- or -CH2-, and A is an optionally substituted, saturated or unsaturated, branched or linear, C1-50 alkylene, cycloalkylene or aromatic group, optionally with one or more carbons within the linear chain being replaced with N, O or S, and wherein the optional substituents are selected from carbonyl, carboxy, hydroxy, amino and other groups, and Y is the covalent linkage between A and Z where Y is selected from -NHCO-, -CONH-, -CONHNHCO-, -N=N-, -N=CH-, -NHCH2-, -NHN=CH-, -NHNHCH2-, -SS-, -SCH2-, -CH2S-, -NHCRNH-, -COO-, -OCO-, and R is O, S or NH2, and Z is GCSF or EPO. The invention also describes reagents that can be used as probes for the detection of buried thiol groups of a protein or peptide, said reagent comprising a complex of either vitamin B12 (or an analogue thereof) or more generally of any instrumentally or visually detectable label, covalently linked to a diradical spacer, said spacer having a terminal reactive group capable of forming a disulphide bond with a free thiol in said protein or peptides.

    专利号:CA-573727-A
    优先权日:
    标 题:Process for the synthesis of 5-hydroxybenzimidazole

    专利号:US-11124609-B2
    优先权日:2016-08-05
    标 题:Polymeric coatings for metal surfaces
    发明人:LAWTON JOHN A
    权利人:SEABOURNE SOLUTIONS LLC
    摘要:Polymer compositions for coating of metal surfaces including moieties that interact with a metal atom in the metal surface and optionally containing antifoulant moieties. These polymer compositions provide lubricious coatings for medical devices, anticorrosion coatings for metal components, and antifoulant coatings for marine components such as propellers. The polymer composition is synthesized in a safe manner in which the synthesis components are added to a synthesis vat and there is no need for filtration or removal of waste materials in any step including the consumer use. As such this invention provides an environmentally sound approach to composition synthesis, formulation development, and consumer use.
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    合成参考文献


    参考文献:10.1007/pl00007067
    摘要:Rajasekaran LR, Blake TJ. New Plant Growth Regulators Protect Photosynthesis and Enhance Growth Under Drought of Jack Pine Seedlings. Journal of Plant Growth Regulation. 1999 Dec;18(4):175–81. doi: 10.1007/pl00007067.
    参考文献:10.1055/s-0030-1259007
    摘要:Hanan E, Chan B, Estrada A, Shore D, Lyssikatos J. Mild and General One-Pot Reduction and Cyclization of Aromatic and Heteroaromatic 2-Nitroamines to Bicyclic 2H-Imidazoles. Synlett. 2010 Oct 14;2010(18):2759–64. doi: 10.1055/s-0030-1259007.
    参考文献:10.1007/978-981-99-6831-2_24
    摘要:Sharma R, Ojha A, Bhunia B. Microbial Production of Vitamin B12 Using Food Matrices. 2023. In: Food Process Engineering and Technology.
    摘要:Luneva OG, Gendel LIa, Kuznetsov IuV, Smirnov LD. [Interaction of nonelectrolytes, the derivatives of 5-hydroxybenzimidazole, with erythrocyte membrane]. Biofizika. 2005 Mar;50(2):310–5.
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