CAS: 56046-36-7; 8-Bromo-3,7-Dihydro-6H-Purin-6-One

该化合物是一种溴化的纯衍生物,在有机合成和制药研究方面有很大用途,其结构是核素类比和其他生物活性化合物的制备中的关键中间体.溴替代物可增强反应性,促进诸如铃木或Buchwald-Hartwig的选择性交叉反应.这种复合物具有很高的纯度和稳定性,适合精确的合成应用.它在改变纯性纸巾对开发有针对性的治疗方法的药用化学作用特别宝贵.建议,在受控制的条件下进行适当处理,因为其可能具有光和湿度的敏感性.

结构式图片

相似化合物

10357-68-3 68-94-0 87781-93-9

上下游产品

8-bromoadenine 8-bromo-2'-deoxyinosine 8-bromo-2'-deoxyadenosine

合成工艺路线路线简述

    📜8-溴腺嘌呤置于三氧化二氮,溶剂黄146体系中,化学反应 1.0H,以61%的收率获得产物8-溴次黄嘌呤
    参考文献:黄嘌呤氧化酶的嘌呤类似物抑制剂-结构活性关系和拟议的钼辅因子结合
    标题:黄嘌呤氧化酶的嘌呤类似物抑制剂-结构活性关系和拟议的钼辅因子结合
    摘要:已经制备了许多新的次黄嘌呤类似物作为黄嘌呤氧化酶的底物抑制剂.最值得一提的抑制新次黄嘌呤类似物是3-(米间-甲苯基)吡唑并[1,5-一个]嘧啶-7-酮(47),Id 50 0.06μ中号和3-苯基吡唑并[1,5-一个]嘧啶-7--酮(46),Id 50 0.40μ M. 5-(p-氯苯基)吡唑并[1,5-一个]嘧啶-7-酮(63)和相应的5-硝基苯基衍生物64表现出id 50的0.21及0.23μ中号,分别.7-苯基吡并[1,5一]-小号-三嗪-4-酮(40)被示出为表现出id 50 0.047μ M.这些新的苯基取代的次黄嘌呤类似物的结构-活性关系进行了讨论,并与比较黄嘌呤类似物3-米甲苯基-和3-苯基-7-羟基[1,5-一个]嘧啶-5-酮(90)和(91),预先从我们的实验室报道具有id 50 0.025 0.038和μ中号,分别.苯基和取代的苯基的存在直接有助于这些有效抑制
    DOI:10.1002/jhet.5570220303

    专利信息


    专利号:US-8618279-B2
    优先权日:2009-01-15
    标 题 :Synthesis of 2′,3′— and 3′,5′—cyclic phosphate mono-and oligonucleotides
    发明人:LAIKHTER ANDREI; SRIVASTAVA SURESH CHANDRA; SRIVASTAVA NAVEEN
    权利人:LAIKHTER ANDREI; SRIVASTAVA SURESH CHANDRA; SRIVASTAVA NAVEEN; CHEMGENES CORP
    摘要:The invention provides a novel method for the chemical synthesis of 2′,3′-cyclic phosphate and phosphorothioate of mono and terminated oligonucleotides synthesis. The invention also provides a novel method of for the chemical synthesis of 2′,3′- and 3′,5′-cyclic phosphate and phosphorothioate mononucleotide nucleotides. The process is based on quick and efficient cyclization of phosphoramidate moiety and neighboring hydroxyl group. The present invention is directed towards the synthesis of high purity DNA and RNAs, specifically to introduce cyclic phosphate at 3′-end of oligonucleotides. Such DNA and RNA's have extensive application in therapeutics, diagnostics, drug design, and selective inhibition of an RNA sequence within cellular environment, in pre-tRNA cleavage and in ribozyme ligation. The 2′,3′-cyclic phosphate nucleosides are involved in a vast number of applications in molecular biology in general and mammalian cells in particular. The invention also envisions providing kits comprising at least one composition disclosed in the present invention.

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    合成参考文献

    参考DOI号:10.1002/jhet.5570220303
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