6-Fluor-bicyclo<3.1.0>hexan | 194864-60-3

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 有机氟化物
• 英文名称: 6-Fluor-bicyclo<3.1.0>hexan
• 英文别名: 6-Fluorobicyclo[3.1.0]hexane
• CAS: 194864-60-3
• 化学式: C₆H₉F
• 分子量: 100.136
• InChiKey: CGRSIAQTWWBUEJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  7
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• Intermediate and process for producing fluorinated carboxylic acid derivative from the same
  申请人：——

  公开号：US20030171431A1

  公开（公告）日：2003-09-11

  The present invention relates to a 2-fluoro-2-(3-oxobicyclopentyl)acetate derivative represented by the formula (1): 1 The compound according to the present invention is useful for efficient syntheses of 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acids.

  本发明涉及一种由化学式（1）表示的2-氟-2-(3-氧代双环戊基)乙酸酯衍生物：1本发明的化合物可用于高效合成2-氨基-6-氟双环[3.1.0]己烷-2,6-二羧酸。
• [EN] 6-FLUOROBICYCLO[3.1.0]HEXANE DERIVATIVES<br/>[FR] DERIVES DE 6-FLUOROBICYCLO[3.1.0]HEXANE
  申请人：TAISHO PHARMA CO LTD

  公开号：WO2003061698A1

  公开（公告）日：2003-07-31

  Antidepressants containing as the active ingredient compounds having group II metabotropic glutamate receptor antagonism; and 2-amino-3-alkoxy-6-fluorobicyclo[3.1.0]- hexane-2,6-dicarboxylic acid derivatives represented by the general formula [I], pharmaceutically acceptable salts thereof, or hydrates of the salts: [I] wherein R1 and R2 may be the same or different from each other and are each hydroxyl, C1-10 alkoxy, or the like; R3 is C1-10 acyl, C1-6 alkoxy-C1-6 acyl, or the like; and R4 and R5 may be the same or different from each other and are each hydrogen, C1-10 alkyl, or the like.

  抗抑郁药物的活性成分包含具有II型代谢型谷氨酸受体拮抗作用的化合物；以及由一般式[I]表示的2-氨基-3-烷氧基-6-氟代双环[3.1.0]-己烷-2,6-二羧酸衍生物，其为药学上可接受的盐或盐的水合物：[I]其中R1和R2可以相同或不同，且均为羟基、C1-10烷氧基或类似物；R3为C1-10酰基、C1-6烷氧基-C1-6酰基或类似物；R4和R5可以相同或不同，且均为氢、C1-10烷基或类似物。
• [EN] 6-FLUOROBICYCLO[3. 1.0]HEXANE DERIVATIVES<br/>[FR] DERIVES DE 6-FLUOROBICYCLO[3. 1.0]HEXANE
  申请人：TAISHO PHARMA CO LTD

  公开号：WO2000012464A1

  公开（公告）日：2000-03-09

  Fluorobicyclo[3.1.0]hexane derivatives represented by general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same wherein R?1 and R2¿ represent each hydrogen, alkyl, cycloalkyl, etc.; and Y?1 and Y2¿ represent each hydrogen, alkylthio, cycloalkylthio, alkoxy, etc., or one of Y?1 and Y2¿ represents hydrogen and the other represents hydroxy, alkoxy, cycloalkoxy, etc., or Y?1 and Y2¿ together represent oxygen or -X(CH¿2?)nX- (wherein X represents oxygen or sulfur; and n is 2 or 3). These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists, in treating and preventing psychiatric disorders such as schizophrenia, anxiety, depression and bipolar disturbance, and neurologic diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's disease, Parkinson's disease, movement disorder in association with muscular rigidity, brain ischemia, brain insufficiency, spinal cord lesion and head disorder.

  通式（I）所代表的氟代双环[3.1.0]己烷衍生物，其药物可接受的盐或水合物，其中R?1和R2¿分别代表氢，烷基，环烷基等；Y?1和Y2¿分别代表氢，烷硫基，环烷硫基，烷氧基等，或者Y?1和Y2¿中的一个代表氢，另一个代表羟基，烷氧基，环烷氧基等，或者Y?1和Y2¿一起代表氧或-X(CH¿2?)nX-（其中X代表氧或硫；n为2或3）。这些化合物在治疗和预防精神障碍，如精神分裂症，焦虑症，抑郁症和双相障碍以及神经疾病，如药物成瘾，认知障碍，阿尔茨海默病，亨廷顿病，帕金森病，与肌肉僵硬相关的运动障碍，脑缺血，脑功能不足，脊髓损伤和头部疾病方面有用，特别是作为第二组代谢型谷氨酸受体激动剂。
• 6-Fluorobicyclo[3.1.0]hexane derivatives
  申请人：Nakazato Atsuro

  公开号：US20050119345A1

  公开（公告）日：2005-06-02

  An antidepressant comprising, as an active ingredient, a compound having an antagonistic effect on group II metabotropic glutamate receptors, as well as a 2-amino-3-alkoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative of Formula [I]: [wherein R 1 and R 2 , which may be the same or different, each represent a hydroxyl group, a C 1-10 alkoxy group, etc.; R 3 represents a C 1-10 acyl group, a C 1-6 alkoxy-C 1-6 acyl group, etc.; and R 4 and R 5 , which may be the same or different, each represent a hydrogen atom, a C 1-10 alkyl group, etc.] or a pharmaceutically acceptable salt or hydrate thereof.

  一种抗抑郁药，包含作为活性成分的一种具有对II类代谢型谷氨酸受体拮抗作用的化合物，以及公式[I]的2-氨基-3-烷氧基-6-氟-双环[3.1.0]己烷-2,6-二羧酸衍生物：[其中R1和R2，可以相同或不同，分别代表羟基，C1-10烷氧基等；R3代表C1-10酰基，C1-6烷氧基-C1-6酰基等；R4和R5，可以相同或不同，分别代表氢原子，C1-10烷基等]或其药学上可接受的盐或水合物。
• 6-FLUOROBICYCLO 3. 1.0]HEXANE DERIVATIVES
  申请人：Taisho Pharmaceutical Co. Ltd.

  公开号：EP1110943A1

  公开（公告）日：2001-06-27

  The present invention provides fluorobicyclo[3.1.0]hexane derivatives represented by the formula [wherein R1 and R2 are the same or different and each represents a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group or a C3-8 cycloalkyl-C1-5 alkyl group: Y1 and Y2 are the same or different and each represents a hydrogen atom, a C1-10 alkylthio group, a C3-8 cycloalkylthio group, a C3-8 cycloalkyl-C1-5 alkylthio group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or one represents a hydrogen atom and the other represents a hydroxyl group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or Y1 and Y2 together represent an oxygen atom or -X(CH2)nX- (X represents an oxygen atom or a sulfur atom: n is 2 or 3) ], pharmaceutically acceptable salts thereof, or hydrates thereof. The compounds of the present invention are useful as drugs, in particular group 2 metabotropic glutamate receptor agonists, and useful for treatment or prevention of psychiatric disorders such as, for example, schizophrenia, anxiety and associated diseases, depression, bipolar disorder, and epilepsy, as well as neurological diseases such as, for example, drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, dyskinesia associated with muscular stiffness, cerebral ischemia, cerebral failure, myelopathy, and head trauma.

  本发明提供了由式表示的氟双环[3.1.0]己烷衍生物 [其中 R1 和 R2 相同或不同，各自代表氢原子、C1-10 烷基、C3-8 环烷基或 C3-8 环烷基-C1-5 烷基：Y1和Y2相同或不同，且各自代表氢原子、C1-10烷硫基、C3-8环烷基硫基、C3-8环烷基-C1-5烷硫基、C1-5烷氧基、C3-8环烷氧基或C3-8环烷基-C1-5烷氧基；或一个代表氢原子，另一个代表羟基、C1-5 烷氧基、C3-8 环烷氧基或 C3-8 环烷基-C1-5 烷氧基；或 Y1 和 Y2 共同代表氧原子或 -X(CH2)nX- （X 代表氧原子或硫原子：n为2或3） ]、其药学上可接受的盐或其水合物。 本发明的化合物可用作药物，尤其是第 2 组代谢型谷氨酸受体激动剂，并可用于治疗或预防精神疾病，例如精神分裂症、焦虑症及相关疾病、抑郁症、双相情感障碍、癫痫以及神经系统疾病、和癫痫，以及神经系统疾病，如药物依赖、认知障碍、阿尔茨海默病、亨廷顿舞蹈症、帕金森病、与肌肉僵硬相关的运动障碍、脑缺血、脑衰竭、脊髓病和头部创伤。