5-fluoro-1-[(2R,5R)-4-hydroxy-5-(hydroxymethyl)-2-oxolanyl]pyrimidine-2,4-dione

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷
• 英文名称: 5-fluoro-1-[(2R,5R)-4-hydroxy-5-(hydroxymethyl)-2-oxolanyl]pyrimidine-2,4-dione
• 英文别名: 5-fluoro-1-[(2R,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
• 化学式: C₉H₁₁FN₂O₅
• 分子量: 246.195
• InChiKey: ODKNJVUHOIMIIZ-JXBXZBNISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  99.1
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• [EN] FLOXURIDINE SYNTHESIS<br/>[FR] SYNTHÈSE DE FLOXURIDINE
  申请人：NUCANA PLC

  公开号：WO2019053476A1

  公开（公告）日：2019-03-21

  The present invention relates to a process for the preparation of floxuridine, said process comprising reacting a compound of Formula la with a compound of Formula lla in the presence of an acid Al to provide a compound of Formula Ilia in substantially diastereomerically pure form. Floxuridine may be useful as an anti-cancer drug. Floxuridine may also be useful in the preparation of other anti-cancer drugs, e.g. NUC-3373.

  本发明涉及一种氟尿嘧啶的制备方法，该方法包括在酸Al的存在下，使式Ia化合物与式IIa化合物发生反应，以提供基本上对映异构纯形式的式IIIa化合物。氟尿嘧啶可能作为一种抗癌药物有用。氟尿嘧啶还可能在制备其他抗癌药物，例如NUC-3373中有用。
• Modified Oligonucleotides and Applications Thereof
  申请人：Mullah Khairuzzaman Bashar

  公开号：US20110144319A1

  公开（公告）日：2011-06-16

  Disclosed, among other things, are primers containing certain modified nucleobases in the 3′ terminal region of the primers that provide reduced formation of primer-dimers during amplification reactions, and various methods of use thereof.

  披露了包含在引物的3'端区域中的某些修饰核苷酸碱基的引物，这些引物在扩增反应过程中减少引物二聚体形成，并且披露了各种使用方法。
• PHOSPHORAMIDATE DERIVATIVES OF 5 - FLUORO - 2` - DEOXYURIDINE FOR USE IN THE TREATMENT OF CANCER
  申请人：McGuigan Christopher

  公开号：US20140057866A1

  公开（公告）日：2014-02-27

  Phosphoramidate derivatives of 5-fluoro-2′-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.

  本发明公开了用于治疗癌症的5-氟-2'-脱氧尿嘧啶的磷酰胺衍生物，特别是用于治疗患有耐药性的癌症的情况，例如，在患有核苷转运蛋白水平降低的细胞、核苷激酶缺陷细胞、支原体感染细胞或胸苷酸合成酶水平升高的细胞的患者中。
• 5'-POSITION DIBENZYL MONOPHOSPHATE DERIVATIVE OF NUCLEOSIDE-BASED ANTICANCER AGENT OR ANTIVIRUS AGENT
  申请人：Ohara Pharmaceutical Co., Ltd.

  公开号：US20200123190A1

  公开（公告）日：2020-04-23

  To provide, in place of injected agents (nucleoside-based anticancer agents or antivirus agents) clinically used as therapeutic drugs for cancer or virus infections, a medicine that has high stability with respect to various hydrolytic metabolic enzymes, is absorbed into the body even by oral administration, and exhibits a cytocidal effect by being incorporated into a DNA and RNA biosynthetic route and inhibiting the modification and extension of DNA and RNA or inhibiting reverse transcriptases or inhibiting protein synthesis. The aforementioned problem is solved by a novel compound represented by formula (I). (In the formula, D is the 5′-position moiety of a nucleoside-based anticancer agent or an antivirus agent, and R 1 and R 2 are each a benzyl group that may have the same substituent or different substituents.)

  提供一种替代核苷酸类抗癌药物或抗病毒药物注射剂的药物，该药物具有对各种水解代谢酶高稳定性，即使口服也能被身体吸收，并通过被纳入到DNA和RNA生物合成途径中并抑制DNA和RNA的修饰和延伸或抑制逆转录酶或抑制蛋白质合成而表现出细胞毒性的特点。上述问题通过一种新化合物（I）来解决。（在公式中，D是核苷酸类抗癌药物或抗病毒药物的5'-位置基团，R1和R2分别是苯甲基，可以具有相同的取代基或不同的取代基。）
• [EN] IBANDRONATE CONJUGATES OF NUCLEOSIDE ANTIMETABOLITES<br/>[FR] CONJUGUÉS D'IBANDRONATE D'ANTIMÉTABOLITES NUCLÉOSIDIQUES
  申请人：MBC PHARMA INC

  公开号：WO2019005207A1

  公开（公告）日：2019-01-03

  Provided herein are conjugates of nucleoside antimetabolites and their analogs with ibandronate, pharmaceutical compositions including one or more of said conjugates, methods of synthesizing the same as well as methods of treating diseases and or conditions using the same.

  本文提供了核苷类抗代谢物及其类似物与伊班膦酸的结合物，包括含有一种或多种该结合物的药物组合物，以及合成该结合物的方法以及使用该结合物治疗疾病和/或病情的方法。