CAS: 7013-16-3; 9-((2R,3S,4S,5R)-3,4-Dihydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)-1H-Purin-6(9H)-One

该化合物是具有显著抗病毒特性的核核素类比,其特点是其纯基结构,特别是经改良的腺素,与阿拉伯甘蔗糖糖糖协会相联系,该化合物展示了一种对生物活动具有重要意义的抗生素结构,Ara-A主要因其对某种病毒感染,特别是因干扰病毒性DNA合成而导致的病毒性病毒感染的有效性而得到承认.该化合物的操作机制包括将其纳入病毒性脱氧核糖核酸,导致在复制过程中链的终止.此外,ARA-A还研究其在其他各种病毒感染和某些癌症中的潜在治疗用途,其溶性及其生物系统中的稳定性对于其作为治疗剂的功效至关重要.总体而言,9-D-Araminusyl-1,9-diHMH-6H-purin-6-one是医药化学的重要化合物,特别是在抗病毒疗法的研制中.

结构式图片

上下游产品

arabinosyl adenine 2,3,5-tri-O-benzyl-1-(4-nitrobenzoyloxy)-D-arabinofuranose 2,3,5-tri-O-benzyl-α-D-arabinofuranosyl chloride 2,3,5-tri-O-benzyl-D-arabinose(2R,3R,4S,5R)-2-(acetoxymethyl)-5-(6-chloro-9H-purin-9-yl)tetrahydrofuran-3,4-diyl diacetate 6-(3-hydroxybenzylamino)-9-β-D-arabinofuranosylpurine S-methyl-L-cysteine 1-methylinosine

合成工艺路线路线简述

    📜鸟嘌呤置于purine Nucleoside 2'-Deoxyribosyltransferase From Trypanosoma Brucei体系中,用 Aq. Phosphate Buffer 作为反应溶剂,化学反应 8.0H,反应生成 阿糖肌苷
    参考文献:使用来自布鲁氏锥虫的高度通用的嘌呤核苷2'-脱氧核糖基转移酶酶促合成治疗性核苷
    标题:使用来自布鲁氏锥虫的高度通用的嘌呤核苷2'-脱氧核糖基转移酶酶促合成治疗性核苷
    摘要:与多步化学方法相比,使用酶来合成核苷类似物具有多个优势,包括化学,区域和立体选择性以及较温和的反应条件.本文报道了来自布鲁氏锥虫的嘌呤核苷2'-脱氧核糖基转移酶(pdt)的生产,表征和利用.tb Pdt是一种二聚体,不仅在很宽的温度范围(50-70oc),Ph(4-7)和离子强度(0-500 Mm Nacl)范围内都显示出出色的活性和稳定性,而且在高温下具有非凡的高稳定性碱性条件(ph 8-10).bpdt被证明可以熟练地合成许多治疗性核苷,包括去羟肌苷,维达拉滨,克拉屈滨,氟达拉滨和奈拉拉滨.用ala或ser进行结构指导的val11置换,导致变体的活性提高了2.8倍.tb Pdt也共价固定在戊二醛激活的磁性微球上.选择了m Tb Pdt3作为最佳衍生物(4200 Iu / G,活性回收率为22%),可以轻松地将其重新捕获和再循环用于> 25个反应,而活性损失可忽略不计.最后,男铽pdt3
    DOI:10.1002/cctc.201800775

    海关参考信息

    专利信息


    专利号:US-11858953-B2
    优先权日:2018-04-04
    标 题:Compositions and methods for synthesis of phosphorylated molecules
    发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT
    权利人:UNIV CALIFORNIA
    摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.

    专利号:US-2005080260-A1
    优先权日:2003-04-22
    标 题 :Preparation of prodrugs for selective drug delivery
    发明人:MILLS RANDELL L; WU GUO-ZHANG
    摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

    专利号:US-2020239500-A1
    优先权日:2018-04-04
    标 题 :Compositions and Methods for Synthesis of Phosphorylated Molecules

    专利号:US-2016312261-A1
    优先权日:2015-04-24
    标 题 :Enzymatic production of cytosinic nucleoside analogues
    发明人:PASCUAL GILABERT MARTA; DERONCELÉ THOMAS VICTOR M; MONTILLA ARÉVALO RAFAEL
    权利人:PLASMIA BIOTECH S L
    摘要:The invention relates to the enzymatic production of cytosinic nucleoside analogues. In particular it relates to a new synthesis process of cytosine nucleoside analogues by using nucleoside phosphorylase enzymes, particularly Pyrimidin Nucleoside Phosphorylases (PyNPs) or mixtures of Purine Nucleoside Phosphorylases (PNPs) and PyNPs.

    专利号:EP-2883959-A1
    优先权日:2013-12-13
    标 题:Enzymatic production of cytosinic nucleoside analogues
    发明人:PASCUAL GILABERT MARTA; DERONCELÉ THOMAS VÃ?CTOR M; MONTILLA ARÉVALO RAFAEL
    权利人:PLASMIA BIOTECH S L
    摘要:The invention relates to a new synthesis process of cytosine nucleoside analogues by using nucleoside phosphorylase enzymes, particularly Pyrimidin Nucleoside Phosphorylases (PyNPs) or mixtures of Purine Nucleoside Phosphorylases (PNPs) and PyNPs.

    专利号:US-2021332070-A1
    优先权日:2018-04-04
    标题:Compositions and Methods for Synthesis of Phosphorylated Molecules

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.3109/02713688609015124
    摘要:O'Brien WJ. Therapy with 9-beta-D-arabinofuranosyladenine (ARA-A) and 2'-deoxycoformycin increases the ARA-A content of ocular tissues. Curr Eye Res. 1986 Aug;5(8):595–9. doi: 10.3109/02713688609015124.
    参考文献:10.1152/ajpheart.1986.250.3.h482
    摘要:Gorman MW, Bassingthwaighte JB, Olsson RA, Sparks HV. Endothelial cell uptake of adenosine in canine skeletal muscle. American Journal of Physiology-Heart and Circulatory Physiology. 1986 Mar 01;250(3):H482–9. doi: 10.1152/ajpheart.1986.250.3.h482.
    参考文献:10.1146/annurev.ph.48.030186.001541|10.1146/annurev.physiol.48.1.321
    摘要:Bassingthwaighte JB, Sparks HV. Indicator Dilution Estimation of Capillary Endothelial Transport. Annu. Rev. Physiol. 1986 Oct;48(1):321–34. doi: 10.1146/annurev.ph.48.030186.001541.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知