1,2-Dihydro-1,4-dimethyl-2-oxo-pyrimidin | 14248-07-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 1,2-Dihydro-1,4-dimethyl-2-oxo-pyrimidin
• 英文别名: 1,4-Dimethyl-2-oxo-1,2-dihydro-pyrimidin；1,4-Dimethylpyrimidin-2(1H)-one；1,4-dimethylpyrimidin-2-one
• CAS: 14248-07-8
• 化学式: C₆H₈N₂O
• 分子量: 124.142
• InChiKey: NNSVNLJVWPLJJA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  32.7
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  1,2-Dihydro-1,4-dimethyl-2-oxo-pyrimidin 在 溴 作用下， 以40%的产率得到1,4-Dimethyl-5-brompyrimid-2-on
  参考文献：
  名称：

  5-Halopyrimid-2-ones

  摘要：

  描述了具有有趣药理特性的嘧啶-2-酮的新衍生物。本发明的化合物已被发现可用于控制和特别是抑制恶性肿瘤和白血病的中期有用。还描述了制备新化合物的方法和含有它们的药物组合物。

  公开号：

  US04395406A1

文献信息

• NOVEL SYNTHESIS OF BETA-NUCLEOSIDES
  申请人：Chu Chi-Yuan

  公开号：US20090124797A1

  公开（公告）日：2009-05-14

  This invention relates to a process of stereoselectively synthesizing β-nucleoside, e.g., 2′-deoxy-2,2′-difluorocytidine.

  这项发明涉及一种立体选择性合成β-核苷的过程，例如2'-脱氧-2,2'-二氟胞嘧啶。
• Nucleoside prodrugs and uses thereof
  申请人：Hecker Scott J.

  公开号：US20090209481A1

  公开（公告）日：2009-08-20

  Compounds having the formula I or II wherein R 1 , R 2 , B, and V are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.

  具有公式I或II的化合物，其中R1、R2、B和V的定义如本文所述，是丙型肝炎病毒NS5b聚合酶抑制剂。还公开了用于治疗HCV感染和抑制HCV复制的组合物和方法。
• BENZAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
  申请人：Hilpert Kurt

  公开号：US20140073651A1

  公开（公告）日：2014-03-13

  The invention relates to benzamide derivatives of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.

  这项发明涉及公式（I）的苯甲酰胺衍生物， 其中R1、R2、R3、R4、R5、R6、n和Y如描述中所定义，它们的制备以及它们作为药用活性化合物的用途。
• Glycopeptide Antibiotic Derivative
  申请人：Nishitani Yasuhiro

  公开号：US20090286717A1

  公开（公告）日：2009-11-19

  The present invention provides a novel glycopeptide antibiotic derivative. These derivatives are represented by the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R A is —X 1 —Ar 1 —X 2 —Y—X 3 —Ar 2 wherein X 1 , X 2 and X 3 are single bond; heteroatom-containing group selected from the group consisting of —N═, ═N—, —NR 1 — (R 1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO 2 —, or a linkage thereof; or alkylene or alkenylene optionally substituted and optionally interrupted by one or more of said heteroatom-containing group; Y is —NR 2 CO—, —CONR 2 — (R 2 is hydrogen or lower alkyl), or a group of the formula (II) wherein R 3 is alkylene; Ar 1 and Ar 2 are a carbocycle or a heterocycle which is optionally substituted and may have an unsaturated bond; R B is —NHNR X R Y or —NR Z OR W wherein R X is hydrogen or lower alkyl; R Y is hydrogen, optionally substituted lower alkyl, C(═NH)NH 2 , CSNH 2 , COCONH 2 , CN, optionally substituted heterocyclic group, and optionally substituted carbamoyl; R Z is hydrogen or lower alkyl; R W is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted heterocyclic group, optionally substituted heterocyclic carbonyl or optionally substituted carbamoyl; R C is hydrogen or optionally substituted alkyl, wherein said alkyl may be interrupted by a heteroatom-containing group selected from N═, ═N—, —NR 1 — (R 1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO 2 —; and R is optionally substituted alkyl.

  本发明提供了一种新型的糖肽抗生素衍生物。这些衍生物由以下式（I）或其药学上可接受的盐或溶剂表示，其中RA为—X1—Ar1—X2—Y—X3—Ar2，其中X1、X2和X3为单键；从—N═、═N—、—NR1—（R1为氢或较低的烷基）、—O—、—S—、—SO—和—SO2—中选择的含有杂原子的基团，或者它们的连接；或者由一个或多个上述含有杂原子的基团选择性取代和选择性中断的烷基或烯基；Y为—NR2CO—、—CONR2—（R2为氢或较低的烷基），或者具有以下式（II）的基团，其中R3为烷基；Ar1和Ar2为可能取代且可能具有不饱和键的碳环或杂环；RB为—NHNRXRY或—NRZORW，其中RX为氢或较低的烷基；RY为氢、选择性取代的较低烷基、C(═NH)NH2、CSNH2、COCONH2、CN、选择性取代的杂环基团和选择性取代的氨基甲酰；RZ为氢或较低的烷基；RW为氢、选择性取代的较低烷基、选择性取代的较低烯基、选择性取代的杂环基团、选择性取代的杂环酰基或选择性取代的氨基甲酰；RC为氢或选择性取代的烷基，其中所述的烷基可以被从—N═、═N—、—NR1—（R1为氢或较低的烷基）、—O—、—S—、—SO—和—SO2—中选择的含有杂原子的基团中断；且R为选择性取代的烷基。
• [EN] TRICYCLIC ANTIBIOTICS<br/>[FR] ANTIBIOTIQUES TRICYCLIQUES
  申请人：BASILEA PHARMACEUTICA AG

  公开号：WO2012171860A1

  公开（公告）日：2012-12-20

  Compounds of formula (I), wherein A1 represents -0-, -S- or -CH2-; A2 represents -CH2- or -0-; A3 represents C3-C8cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen or oxygen, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, -C(=0)-; G represents aryl or heteroaryl, which is unsubstituted or substituted; X1 represents a nitrogen atom or CR1; R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom; m is 0 or 1; n is 1; the -(CH2)n- group is unsubstituted or substituted; p is 0 or 1; or pharmaceutically acceptable salts thereof are valuable for use as a medicament for the treatment of bacterial infections.

  式(I)的化合物，其中A1代表-O-，-S-或-CH2-；A2代表- -或-O-；A3代表C3-C8环烷基，饱和或不饱和的含有1、2或3个氮或氧杂原子的4到8元杂环二基，其中A3基未取代或取代；A4代表C1-C4烷基，-C(=0)-；G代表芳基或杂芳基，未取代或取代；X1代表氮原子或CR1；R1代表氢原子或卤原子；R2代表氢原子；m为0或1；n为1；-( )n-基未取代或取代；p为0或1；或其在药学上可接受的盐，用作治疗细菌感染的药物。