CAS: 41398-85-0; 5-Methylpyrimidin-2(1H)-One

该化合物是一种七环有机化合物,其五级为五级,以甲基组替代一个火利米丁核心,二级为氢氧基,其盐质为盐盐,该化合物因其反应性pyrimidine scffold,在制药和农用化学合成中具有多种用途的中间体.盐质形式增强了溶性与稳定性,便利了处理和储存.其结构特征使得它对于建造生物活性分子很有价值,特别是在研制核核素类比和酶抑制剂方面.该化合物表现出很高的纯度和一贯性能,确保研究和工业应用的可靠性.其定义明确的化学特性使得能够精确地修改定向合成途径.

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CAS号342909-55-1 3-Ethoxy-2-meth... | CAS号57-13-6 尿素 | CAS号4744-08-5 丙醛二乙基乙缩醛 | CAS号68-12-2 N,N-二甲基甲酰胺 | CAS号41398-85-0 2-羟基-5-甲基嘧啶 | CAS号16002-19-0 Propanedial, 2-... | CAS号22003-31-2 1-[(2S,4S,5R)-4... | CAS号1363821-21-9 ((2R,3S,5R)-3-h... | CAS号41398-85-0 2-羟基-5-甲基嘧啶

合成工艺路线路线简述

    1-(3-O-Levulinyl-2-Deoxy-β-D-Ribofuranosyl)-5-Methyl-2-Pyrimidinone置于吡啶,四氮唑,盐酸,Ammonium Hydroxide,水,碘,溶剂黄146,Sodium Hydroxide体系中,用 四氢呋喃,水,乙腈 作为反应溶剂,化学反应 12.17H,反应生成 2-羟基-5-甲基嘧啶
    参考文献:含(6-4)个光产物的dna的碱降解机理†
    标题:含(6-4)个光产物的dna的碱降解机理†
    摘要:(6-4)光产物是紫外线在dna中产生的主要受损碱基之一.已知该损伤是碱不稳定的,当用热碱处理紫外线照射的dna时,在其部位会发生链断裂.我们已经分析了通过碱处理得到的产品.二磷酸核苷通过HPLC,NMR光谱和质谱分析,含有(6-4)个光产物.我们先前发现5'组分的n3-C4键通过弱碱处理而水解,并且本研究表明以下反应是3'组分上糖苷键的水解.即使不存在3'侧翼核苷酸,该成分的糖部分也会丢失.对于二聚体和三聚体,还观测到糖苷键水解.5-甲基-2-嘧啶酮,它被用作(6-4)光产物的3'成分的类似物,并阐明了其机理.最后,对四聚物d(gt(6-4)tc)进行碱处理,得到了2'-脱氧胞苷5'-单磷酸酯,尽管 2'-脱氧鸟苷3'-单磷酸酯未检测到.该结果证明了(6-4)光产物3'组分上糖苷键的水解以及随后的β消除导致链断裂.还显示出,杜瓦价异构体3'组分的糖苷键比(6-4)光产物的碱不稳定.
    DOI:10.1039/c2Ob06966K

    专利信息


    专利号:WO-2024137329-A1
    优先权日:2022-12-20
    标 题:Methods for the synthesis of complement factor d inhibitors and intermediates thereof
    发明人:HASHIMOTO AKIHIRO; TIPPARAJU SURESH KUMAR
    权利人:ALEXION PHARMA INC
    摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.

    专利号:US-8093397-B2
    优先权日:2001-07-03
    标 题:Activators for oligonucleotide synthesis
    发明人:SINHA NANDA; ZEDALIS WILLIAM EDWARD; MIRANDA GREGORY KEITH
    权利人:SINHA NANDA; ZEDALIS WILLIAM EDWARD; MIRANDA GREGORY KEITH; AVECIA BIOTECHNOLOGY INC
    摘要:A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1λ6-benzo[d]isothiazol-3-one, preferably in the presence of an organic base. The 1,1-dioxo-1,2-dihydro-1λ6-benzo[d]isothiazol-3-one is represented by the following structural formula: wherein p is 0 or an integer from 1 to 4; X7 is O or S; R for each occurrence is a substituent, preferably each independently, a halo, a substituted or unsubstituted aliphatic group, —NR11R12, —OR13, —OC(O)R13, —C(O)OR13, or cyano; or two adjacent R groups taken together with the carbon atoms to which they are attached form a six membered saturated or unsaturated ring; R11 and R12 are each, independently, —H, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; and R13 is a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group. Preferred organic bases are pyridine, 3-methylpyridine, or N-methylimidazole.

    专利号:US-2012149888-A1
    优先权日:2009-02-22
    标 题:Synthesis of ara-2'-o-methyl-nucleosides, corresponding phosphoramidites and oligonucleotides incorporating novel modifications for biological application in therapeuctics, diagnostics, g- tetrad forming oligonucleotides and aptamers
    发明人:SRIVASTAVA SURESH C; PANDEY DIVYA; SRIVASTAVA NAVEEN P; SRIVASTAVA ALOK
    权利人:SRIVASTAVA SURESH C; PANDEY DIVYA; SRIVASTAVA NAVEEN P; SRIVASTAVA ALOK
    摘要:The present invention relates to synthesis, purification and methods to obtain high purity novel 2′-arabino-O-methyl nucleosides and the corresponding phosphoramidites of various arabinonucleoside bases and introduction of such units into defined sequence synthetic DNA and RNA. Various synthetic oligonucleotides, such as HIV integrase inhibitor 14-mer and thrombin binding oligonucleotide, thrombin-1, bearing ara-2′-omethyl modification have been synthesized. It is anticipated the oligonucleotides incorporating these monomers will exhibit biological activities related to antisense approach approach, design of better SiRNA's, diagnostic agents. Similarly, it is anticipated that oligonucleotides incorporating such novel nucleosides will be useful to develop therapeutic candidates designing stable G-quadruplexes and Aptamers for oligonucleotide structure, folding topology, evaluation of biochemical properties and design and develop as therapeutic agents. It is further anticipated that the nucleosides, phosphates and triphosphates of this invention could develop as therapeutic agents.

    专利号:US-7635772-B2
    优先权日:2002-12-18
    标 题 :Process for the preparation of oligonucleotides
    发明人:MCCORMAC PAUL
    权利人:AVECIA BIOTECHNOLOGY INC
    摘要:A process for the synthesis of an oligonucleotide is provided in which an oligonucleotide is assembled on a swellable solid support using the phosphoramidite approach in the presence of an activator, wherein the activator is not tetrazole or a substituted tetrazole. Preferred activators are pyridinium, imidazolinium and benzimidazolinium salts; benzotriazole and derivatives thereof; and saccharin or a saccharin derivative. Preferred swellable solid supports comprise functionalised polystyrene, partially hydrolysed polyvinylacetate or poly(acrylamide).

    专利号:US-2016130259-A1
    优先权日:2013-06-24
    标题 :Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
    发明人:LIU HONG; DAI XING; PALANI ANANDAN; HE SHUWEN; NARGUND RAVI; XIAO DONG; DANG QUN; PENG XUANJIA; LI PENG
    权利人:MERCK SHARP & DOHME
    摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

    专利号:US-8344118-B2
    优先权日:2007-10-31
    标 题 :Preparation and isolation of 5′ capped MRNA
    发明人:KORE ANILKUMAR; MUTHIAN SHANMUGASUNDARAM; CHARLES IRUDAYA
    权利人:APPLIED BIOSYSTEMS LLC; KORE ANILKUMAR; MUTHIAN SHANMUGASUNDARAM; CHARLES IRUDAYA
    摘要:The synthesis of capped/tagged RNA, methods of use and kits providing same are contemplated. Tagged RNA permits isolation of RNA transcripts in vitro. The ability to isolate and purify capped RNA results in improved transcription and translation and provides a tool for identifying RNA-protein interactions. Such capped RNA finds use in therapeutic applications, diagnosis and prognosis and in the treatment of cancers and HIV.
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    合成参考文献


    参考文献:10.1562/2006-04-03-ra-866
    摘要:Kistler KA, Matsika S. The fluorescence mechanism of 5-methyl-2-pyrimidinone: an ab initio study of a fluorescent pyrimidine analog. Photochem Photobiol. 2007 May;83(3):611–24. doi: 10.1562/2006-04-03-ra-866.
    参考文献:10.1063/1.2932102
    摘要:Kistler KA, Matsika S. Three-state conical intersections in cytosine and pyrimidinone bases. J Chem Phys. 2008 Jun 07;128(21):215102. doi: 10.1063/1.2932102.
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