5-(4-cyclohexyl-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine | 1058159-02-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 5-(4-cyclohexyl-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine
• 英文别名: (5)-5-(4-Cyclohexyl-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine；5-[(4-cyclohexylphenoxy)methyl]-4,5-dihydro-1,3-oxazol-2-amine
• CAS: 1058159-02-6
• 化学式: C₁₆H₂₂N₂O₂
• 分子量: 274.363
• InChiKey: OJIYDSRHLPPLHH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  56.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-丁炔酸乙酯 、 5-(4-cyclohexyl-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine 在 silica gel 、 dichloromethane ethanol 作用下， 以 乙醇 为溶剂， 反应 1.33h， 以to afford 190 mg of 2-(4-cyclohexyl-phenoxymethyl)-5-methyl-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-one as a white solid的产率得到2-(4-cyclohexyl-phenoxymethyl)-5-methyl-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-one
  参考文献：
  名称：

  SUBSTITUTED DIHYDRO AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF

  摘要：

  本发明涉及一系列取代二氢和四氢噁唑嘧啶酮，具体地，涉及一系列式(I)的2-取代-2,3-二氢噁唑并[3,2-a]嘧啶-7-酮和2-取代-2,3,5,6-四氢噁唑并[3,2-a]嘧啶-7-酮：其中p，n，X，Y，R1，R2，R3，R4，R5，R6，R7和R8如所定义。本发明还涉及制备这些化合物的方法，包括新型中间体。本发明的化合物是代谢型谷氨酸受体(mGluR)的调节剂，特别是mGluR2受体。因此，本发明的化合物在制药领域中有用，特别是在治疗和/或预防各种中枢神经系统疾病(CNS)，包括但不限于急性和慢性神经退行性疾病、精神病、惊厥、焦虑、抑郁、偏头痛、疼痛、睡眠障碍和呕吐等方面。

  公开号：

  US20100075994A1

文献信息

• [EN] SUBSTITUTED PHENOXYMETHYL DIHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF<br/>[FR] PHÉNOXYMÉTHYL-DIHYDRO-OXAZOLOPYRIMIDINONES SUBSTITUÉES, LEUR PRÉPARATION ET LEUR UTILISATION
  申请人：SANOFI AVENTIS

  公开号：WO2011034832A1

  公开（公告）日：2011-03-24

  The present invention relates to a series of substituted phenoxymethyl dihydro oxazolopyrimidinones of formula (I) defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

  本发明涉及一系列被取代的苯氧甲基二氢噁唑吡咯嘧啶酮化合物，其化学式为（I）。本发明还涉及制备这些化合物的方法，包括新颖的中间体。本发明的化合物是代谢型谷氨酸受体（mGluR）的调节剂，特别是mGluR2受体。因此，本发明的化合物可用作药物制剂，特别是在治疗和/或预防各种中枢神经系统疾病（CNS）方面，包括但不限于急性和慢性神经退行性疾病、精神病、认知缺陷疾病、癫痫、焦虑、抑郁、偏头痛、疼痛、睡眠障碍和呕吐。
• SUBSTITUTED DIHYDRO, TRIHYDRO AND TETRAHYDRO CYCLOALKYLOXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
  申请人：KOSLEY, JR. Raymond Walter

  公开号：US20110077257A1

  公开（公告）日：2011-03-31

  The present disclosure relates to a series of 2-substituted-di- tri or tetra-hydro-8H-cyclopentaoxazolo[3,2-a]pyrimidin-8-ones and 2-substituted-di-, tetra-, or hexa-hydro-cyclohexaoxazolo[3,2-a]pyrimidin-9-ones of formula (I): wherein p, n, A, B, X, Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

  本公开涉及一系列式(I)的2-取代-二、三或四氢-8H-环戊氧唑[3,2-a]嘧啶-8-酮和2-取代-二、四或六氢-环己氧唑[3,2-a]嘧啶-9-酮，其中p，n，A，B，X，Y，R1，R2，R3，R4，R5，R6，R7和R8如本文所定义。本发明还涉及制备这些化合物的方法，包括新的中间体。本发明的化合物是代谢型谷氨酸受体（mGluR）的调节剂，特别是mGluR2受体。因此，本发明的化合物在治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经退行性疾病，精神病，惊厥，焦虑，抑郁，偏头痛，疼痛，睡眠障碍和呕吐方面是有用的药物。
• [EN] SUBSTITUTED DIHYDRO, TRIHYDRO AND TETRAHYDRO CYCLOALKYLOXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF AS ALLOSTERIC MODULATORS OF MGLUR<br/>[FR] DIHYDRO-, TRIHYDRO- ET TÉTRAHYDRO- CYCLOALKYLOXAZOLOPYRIMIDINONES SUBSTITUÉES, PRÉPARATION ET UTILISATION DE CELLES-CI EN TANT QUE  MODULATEURS ALLOSTÉRIQUES DE MGLUR
  申请人：SANOFI AVENTIS

  公开号：WO2009110901A1

  公开（公告）日：2009-09-11

  The present invention relates to a series of 2-substituted-di- tri or tetra-hydro-8H-cyclopentaoxazolo[3,2-a]pyrimidin-8-ones and 2-substituted-di-, tetra-, or hexa-hydro-cyclohexaoxazolo[3,2-a]pyrimidin-9-ones of formula (I). Wherein p, n, A, B, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

  本发明涉及一系列公式（I）的2-取代二，三或四氢-8H-环戊氧唑[3,2-a]嘧啶-8-酮和2-取代二，四或六氢-环己氧唑[3,2-a]嘧啶-9-酮。其中p，n，A，B，X，Y，R1，R2，R3，R4，R5，R6，R7和R8如所定义。本发明还涉及制备这些化合物的方法，包括新颖的中间体。本发明的化合物是代谢型谷氨酸受体（mGluR）的调节剂，特别是mGluR2受体。因此，本发明的化合物在医药学上是有用的，特别是在治疗和/或预防多种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经退行性疾病，精神病，惊厥，焦虑，抑郁，偏头痛，疼痛，睡眠障碍和呕吐等方面。
• Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof
  申请人：Cao Bin

  公开号：US08642603B2

  公开（公告）日：2014-02-04

  The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

  本发明涉及一系列取代的二氢和四氢噁唑嘧啶酮，具体地说，涉及一系列式(I)的2-取代-2,3-二氢噁唑并[3,2-a]嘧啶-7-酮和2-取代-2,3,5,6-四氢噁唑并[3,2-a]嘧啶-7-酮，其中p，n，X，Y，R1，R2，R3，R4，R5，R6，R7和R8如本文所定义。本发明还涉及制备这些化合物的方法，包括新的中间体。本发明的化合物是代谢型谷氨酸受体（mGluR）的调节剂，特别是mGluR2受体。因此，本发明的化合物在制药领域中有用，特别是在治疗和/或预防各种中枢神经系统疾病（CNS）方面，包括但不限于急性和慢性神经退行性疾病、精神病、惊厥、焦虑、抑郁、偏头痛、疼痛、睡眠障碍和呕吐。
• SUBSTITUTED DIHYDRO, TRIHYDRO AND TETRAHYDRO CYCLOALKYLOXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF AS ALLOSTERIC MODULATORS OF MGLUR
  申请人：Sanofi-Aventis

  公开号：EP2268645A1

  公开（公告）日：2011-01-05