2-氨基-5,6-二氯-3,4-二氢喹唑啉 | 444904-63-6

• 物质功能分类: 分析化学 - 标准品 - 药典标准品和杂质标准品
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 2-氨基-5,6-二氯-3,4-二氢喹唑啉
• 英文名称: RL 603
• 英文别名: 2-amino-5,6-dichloro-3,4-dihydroquinazoline；RL603；5,6-dichloro-1,4-dihydroquinazolin-2-amine
• CAS: 444904-63-6
• 化学式: C₈H₇Cl₂N₃
• 分子量: 216.07
• InChiKey: VBKOTIVQMCTTAQ-UHFFFAOYSA-N

物化性质

• 熔点：
  205 - 208oC
• 沸点：
  357.5±52.0 °C(Predicted)
• 密度：
  1.67±0.1 g/cm3(Predicted)
• 溶解度：
  可溶于DMSO（少许）、甲醇（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  50.4
• 氢给体数：
  2
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2-氨基-5,6-二氯-3,4-二氢喹唑啉 、 1,3-二硫烷-2-甲酸乙酯 在 sodium hydride 作用下， 以 四氢呋喃 为溶剂， 生成 N-(5,6-dichloro-1,4-dihydroquinazolin-2-yl)-1,3-dithiolane-2-carboxamide
  参考文献：
  名称：

  Quinazoline derivatives useful for the treatment of peripheral arterial disease and as phosphodiesterase inhibitors

  摘要：

  根据本发明，提供了一种治疗宿主外周动脉疾病的方法，包括向宿主投与式(I)到式(III)或其类似物的治疗有效量的化合物。

  公开号：

  US20060030574A1
• 作为产物：
  描述：

  溴化氰 、 2-氨甲基-3,4-二氯苯胺 以 甲苯 为溶剂， 生成 2-氨基-5,6-二氯-3,4-二氢喹唑啉
  参考文献：
  名称：

  Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: Structure–activity relationship elucidation

  摘要：

  The optimisation of affinity and selectivity in a novel series of dual 5-HT5A/5-HT7 receptor ligands is described. Brain penetrant 2-aminodihydroquinazolines with low nanomolar affinities were identified. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.10.080

文献信息

• 2-AMINO-5,6-DIHALO-3,4-DIHYDROQUINAZOLINES WITH BLOOD PLATELET REDUCING PROPERTIES
  申请人：——

  公开号：US20030114673A1

  公开（公告）日：2003-06-19

  Compounds of formula (E) (wherein X and Y, which may be the same or different, each represents Cl, Br or F) and tautomers thereof have been found to have enhanced platelet count reducing properties. Also provided are methods for synthetically making the compounds of formula (E) and pharmaceutically acceptable addition salts thereof and a method of reducing the platelet count in patient by administering to the patient a platelet reducing effective amount of a compound of formula (E) preferably together with a pharmaceutically acceptable carrier. A pharmaceutical composition is also provided which contains a compound of formula (E) as the active ingredient together with pharmaceutically acceptable excipients. Further provided is a compound of formula (E) for use in therapy and the use of a compound of formula (E) for preparing a medicament for reducing platelet count in a patient.

  化学式为（E）的化合物（其中X和Y，可以相同或不同，分别代表Cl、Br或F）及其互变异构体已被发现具有增强的减少血小板计数的性质。同时提供了合成化学式（E）的化合物及其药学上可接受的盐的方法，以及通过向患者注射化学式（E）的化合物的减少血小板计数的方法，最好与药学上可接受的载体一起使用。还提供了一种含有化学式（E）的化合物作为活性成分的药物组合物，以及药学上可接受的辅料。此外，还提供了一种用于治疗的化学式（E）的化合物，以及用于制备减少患者血小板计数的药物的化学式（E）的化合物的用途。
• Controlled release compositions of agents that reduce circulating levels of platelets and methods therefor
  申请人：Glidden Paul F.

  公开号：US20090324710A1

  公开（公告）日：2009-12-31

  Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal or to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.

  提供了预防和治疗方法，用于通过给予药剂，包括anagrelide和anagrelide衍生物，将循环血小板数量降至低于正常水平或低于正常水平，以抑制血管闭塞事件，包括栓塞。提供了包含这些药剂的方法和制药制剂。
• 2-amino-5,6-dichloro-3,4-dihydroquinazoline, its method of making and using and pharmaceutical compositions thereof
  申请人：Roberts Laboratories Inc.

  公开号：US06194420B1

  公开（公告）日：2001-02-27

  The compound 2-amino-5,6-dichloro-3,4-dihydroquinazoline has been found to have enhanced platelet count reducing properties. Also provided are methods for synthetically making the compound and a method of reducing the platelet count in a patient by administering to the patient a platelet reducing effective amount of the compound preferably together with a pharmaceutically acceptable carrier. A pharmaceutical composition is also provided which contains the above compound as the active ingredient together with pharmaceutically acceptable excipients.

  化合物2-氨基-5,6-二氯-3,4-二氢喹唑啉已被发现具有增强的减少血小板计数的属性。此外，还提供了合成该化合物的方法以及通过向患者施用该化合物的减少血小板计数的有效量的方法，最好与药学上可接受的载体一起使用。还提供了一种药物组合物，其中包含上述化合物作为活性成分，以及药学上可接受的辅料。
• CONTROLLED RELEASE COMPOSITIONS OF AGENTS THAT REDUCE CIRCULATING LEVELS OF PLATELETS AND METHODS THEREFOR
  申请人：Glidden Paul F.

  公开号：US20130022671A1

  公开（公告）日：2013-01-24

  Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal or to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.

  提供了预防和治疗方法，以抑制血管闭塞事件，包括栓塞，通过给予药物，包括阿格列酯和阿格列酯衍生物，将循环血小板数量降低到低于正常水平或低于正常水平的水平。提供了包含这些药物的方法和制药制剂。
• Method of treating hypertension
  申请人：Cipla Limited

  公开号：US10022377B2

  公开（公告）日：2018-07-17

  Disclosed herein are compositions and methods for the treatment of pulmonary hypertension, including pulmonary arterial hypertension. The methods include administering to a patient in need thereof an effective amount of anagrelide or derivative thereof. The compositions include an effective amount of anagrelide or derivative thereof, in some instances combined with one or more additional agents for the treatment of pulmonary hypertension.

  本文公开了治疗肺动脉高压等肺动脉高压的组合物和方法。这些方法包括向有需要的患者施用有效量的阿那格雷或其衍生物。组合物包括有效量的阿那格雷或其衍生物，在某些情况下与一种或多种治疗肺动脉高压的附加制剂结合使用。