3,4-Dihydro-2H-pyrido<1,2-α>pyrimidine hydrochloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 3,4-Dihydro-2H-pyrido<1,2-α>pyrimidine hydrochloride
• 英文别名: 1,2,3,4-tetrahydro-pyrido[1,2-a]pyrimidinylium；1,2,3,4-Tetrahydropyrido[1,2-a]pyrimidin-5-ium
• 化学式: C₈H₁₁N₂
• 分子量: 135.189
• InChiKey: WJEHYVLQWVIEJM-UHFFFAOYSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  15.9
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• PROCESS
  申请人：Zajac Matthew Allen

  公开号：US20110015390A1

  公开（公告）日：2011-01-20

  The present invention generally relates to a novel process for preparing vitronectin receptor antagonist compounds having a benzodiazepinyl core structure. This invention relates to the preparation of pharmaceutically active compounds which inhibit the vitronectin receptor and are useful for treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporosis. In particular, the present invention relates to a novel process for preparing (±)-3-oxo-8-[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid, (R)-3-oxo-8-[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid and (S)-3-oxo-8-[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid or a pharmaceutically acceptable salt thereof.

  本发明涉及一种新型制备具有苯二氮平核心结构的玻璃蛋白受体拮抗剂化合物的方法。本发明涉及制备药物活性化合物，该化合物抑制玻璃蛋白受体，可用于治疗炎症、癌症和心血管疾病，如动脉粥样硬化和再狭窄，以及骨吸收是因素的疾病，如骨质疏松症。特别是，本发明涉及一种新型制备(±)-3-氧代-8-[3-(吡啶-2-基氨基)丙基]氧基}-2-(2,2,2-三氟乙基)-2,3,4,5-四氢-1H-2-苯并唑-4-乙酸，(R)-3-氧代-8-[3-(吡啶-2-基氨基)丙基]氧基}-2-(2,2,2-三氟乙基)-2,3,4,5-四氢-1H-2-苯并唑-4-乙酸和(S)-3-氧代-8-[3-(吡啶-2-基氨基)丙基]氧基}-2-(2,2,2-三氟乙基)-2,3,4,5-四氢-1H-2-苯并唑-4-乙酸或其药学上可接受的盐的方法。
• US8076475B2
  申请人：——

  公开号：US8076475B2

  公开（公告）日：2011-12-13
• [EN] PROCESS<br/>[FR] PROCÉDÉ
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2009111679A2

  公开（公告）日：2009-09-11

  The present invention generally relates to a novel process for preparing vitronectin receptor antagonist compounds having a benzodiazepinyl core structure. This invention relates to the preparation of pharmaceutically active compounds which inhibit the vitronectin receptor and are useful for treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporosis. In particular, the present invention relates to a novel process for preparing (±)-3-oxo-8-[3-(pyridin-2-ylamino)propyl]oxy}- 2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid, (R)-3-oxo-8- [3-(pyridin-2-ylamino) propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2- benzazepine-4-acetic acid and (S)-3-oxo-8-[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2- trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid or a pharmaceutically acceptable salt thereof.