[5-chloro-6-(2-chloro-6-fluorophenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]methanol

• 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: [5-chloro-6-(2-chloro-6-fluorophenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]methanol
• 英文别名: [5-Chloro-6-(2-chloro-6-fluorophenyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]methanol
• 化学式: C₁₂H₇Cl₂FN₄O
• 分子量: 313.118
• InChiKey: IWRNEYVKAJXLDB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  63.3
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Substituted-triazolopyrimidines as anticancer agents
  申请人：American Home Products Corporation

  公开号：US20020068744A1

  公开（公告）日：2002-06-06

  The invention provides a method of treating or inhibiting the growth of cancerous tumour cells and associated diseases in a mammal in need thereof which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof and further provides a method of treating or inhibiting the growth of cancerous tumour cells and associated diseases in a mammal in need thereof by interacting with tubulin and microtubules and promoting microtubule polymerization which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof.

  该发明提供了一种治疗或抑制哺乳动物体内癌症肿瘤细胞及相关疾病的方法，包括向该哺乳动物体内施用有效量的取代三唑吡啶衍生物或其药学上可接受的盐，并进一步提供了一种通过与微管蛋白和微管相互作用并促进微管聚合的方法，治疗或抑制哺乳动物体内癌症肿瘤细胞及相关疾病，包括向该哺乳动物体内施用有效量的取代三唑吡啶衍生物或其药学上可接受的盐。
• A process and intermediates for the preparation of fungicidal 7-alkyl-triazolopyrimidines
  申请人：BASF AKTIENGESELLSCHAFT

  公开号：EP1359150A2

  公开（公告）日：2003-11-05

  A process and intermediates for the preparation of triazolopyrimidine compounds of formula I wherein R1, X, L1, L2, L3, L4 and L5 are as defined in the description, which comprises reacting alkyl 2-aryl-3-alkyl-3-oxopropionates of formula IV wherein R1 and L1, L2, L3, L4 and L5 are as defined for formula I and R' represents an optionally substituted alkyl group, a) with 2-amino-[1,3,4]-triazole, and treating the resulting 5-hydroxytriazolopyrimidines of formula I, wherein X represents a hydroxy group, with a halogenating agent, and b) optionally treating the resulting 5-hydroxytriazolopyrimidines with an alcohol or a thioalkohol in the presence of a base, or with a metal amide, a metal alkyl amide or a metal dialkylamide, or a metal cyanide.

  一种制备式 I 的三唑并嘧啶化合物的工艺和中间体 其中 R1、X、L1、L2、L3、L4 和 L5 如说明中所定义，包括使式 IV 的 2-芳基-3-烷基-3-氧代丙酸烷基酯反应 其中 R1 和 L1、L2、L3、L4 和 L5 如式 I 所定义，R'代表任选取代的烷基、 a) 用 2-氨基-[1,3,4]-三唑，并用卤化剂处理所得到的式 I 的 5-羟基三唑嘧啶，其中 X 代表羟基，以及 b) 可选择在碱存在下用醇或硫代烷醇，或用金属酰胺、金属烷基酰胺或金属二烷基酰胺，或金属氰化物处理所得的 5-羟基三唑并嘧啶。
• SUBSTITUTED-TRIAZOLOPYRIMIDINES AS ANTICANCER AGENTS
  申请人：Wyeth

  公开号：EP1307200A2

  公开（公告）日：2003-05-07
• US7329663B2
  申请人：——

  公开号：US7329663B2

  公开（公告）日：2008-02-12
• [EN] SUBSTITUTED-TRIAZOLOPYRIMIDINES AS ANTICANCER AGENTS<br/>[FR] TRIAZOLOPYRIMIDINES SUBSTITUES COMME AGENTS ANTICANCEREUX
  申请人：AMERICAN HOME PROD

  公开号：WO2002002563A2

  公开（公告）日：2002-01-10

  The invention provides a method of treating of inhibiting the growth of cancerous tumour cells and associated diseases in a mammal in need thereof which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof and further provides a method of treating or inhibiting the growth of cancerous tumour cells and associated diseases in a mammal in need thereof by interacting with tubulin and microtubules and promoting microtubule polymerization which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof.