1-(4-Benzyloxyphenyl)-2-(4-methoxyphenyl)ethan-1-one | 187989-19-1

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: 1-(4-Benzyloxyphenyl)-2-(4-methoxyphenyl)ethan-1-one
• 英文别名: 1-(4-(benzyloxy)phenyl)-2-(4-methoxyphenyl)ethanone；2-(4-methoxyphenyl)-1-(4-phenylmethoxyphenyl)ethanone
• CAS: 187989-19-1
• 化学式: C₂₂H₂₀O₃
• 分子量: 332.399
• InChiKey: YUFHIWUSDCSMDN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  25
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.136
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(4-Benzyloxyphenyl)-2-(4-methoxyphenyl)ethan-1-one 在 palladium(II) hydroxide potassium tert-butylate 、 氢气 、 potassium carbonate 作用下， 以 四氢呋喃 、 甲醇 、 乙腈 为溶剂， 反应 33.5h， 生成 4-(4-methoxyphenyl)-2,2-dimethyl-5-(4-(quinolin-2-ylmethoxy)phenyl)furan-3(2H)-one
  参考文献：
  名称：

  [EN] 1, 2 DISUBSTITUTED HETEROCYCLIC COMPOUNDS
  [FR] COMPOSÉS HÉTÉROCYCLIQUES À SUBSTITUTION EN 1,2

  摘要：

  描述了一种抑制磷酸二酯酶10的1,2-二取代杂环化合物。还描述了这些化合物在治疗哺乳动物，包括人类的中枢神经系统（CNS）疾病和可能影响CNS功能的其他疾病中的过程、药物组成、药物制剂和药物用途。可以治疗的疾病包括神经病、神经退行性疾病和精神疾病，包括但不限于与认知缺陷或精神分裂症症状相关的疾病。

  公开号：

  WO2009158393A1
• 作为产物：
  描述：

  对羟基苯乙酸乙酯 在 水 、 potassium carbonate 、 sodium hydroxide 作用下， 以 甲醇 、 乙腈 为溶剂， 反应 6.0h， 生成 1-(4-Benzyloxyphenyl)-2-(4-methoxyphenyl)ethan-1-one
  参考文献：
  名称：

  [EN] 1, 2 DISUBSTITUTED HETEROCYCLIC COMPOUNDS
  [FR] COMPOSÉS HÉTÉROCYCLIQUES À SUBSTITUTION EN 1,2

  摘要：

  描述了一种抑制磷酸二酯酶10的1,2-二取代杂环化合物。还描述了这些化合物在治疗哺乳动物，包括人类的中枢神经系统（CNS）疾病和可能影响CNS功能的其他疾病中的过程、药物组成、药物制剂和药物用途。可以治疗的疾病包括神经病、神经退行性疾病和精神疾病，包括但不限于与认知缺陷或精神分裂症症状相关的疾病。

  公开号：

  WO2009158393A1

文献信息

• Inhibitor of cox
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：US20040157891A1

  公开（公告）日：2004-08-12

  A compound of the formula (I): 1 wherein R 1 is cycloalkyl, etc; R 2 is (lower)alkoxy, etc; R 3 is (lower)alkylene, etc; R 4 is (lower)alkylene, etc; R 5 is hydroxy, etc; X is “O”, “S”, “SO”, or “SO 2 ”; Y is “CH” or “N”; n is 0 or 1; or pharmaceutically acceptable salts thereof, which are useful as a medicament.

  一种具有以下式（I）的化合物：其中R1是环烷基等；R2是（较低）烷氧基等；R3是（较低）烷基烯基等；R4是（较低）烷基烯基等；R5是羟基等；X为“O”、“S”、“SO”或“SO2”；Y为“CH”或“N”；n为0或1；或其药学上可接受的盐，可用作药物。
• [EN] OXAZOLE DERIVATIVES AS INHIBITORS OF CYCLOOXYGENASE<br/>[FR] DERIVES D'OXAZOLE UTILISES COMME INHIBITEURS DE LA CYCLO-OXYGENASE
  申请人：FUJISAWA PHARMACEUTICAL CO

  公开号：WO2004065374A1

  公开（公告）日：2004-08-05

  A compound of the formula (I): wherein R1 is cycloalkyl, etc; R2 is (lower)alkoxy, etc; R3 is (lower)alkylene, etc; R4 is (lower)alkylene, etc; R5 is hydroxy, etc; X is '0', 'S', 'SO', or 'S02'; Y is 'CH' or 'N'; n is 0 or 1; or pharmaceutically acceptable salts thereof, which are useful as a medicament.

  其中R1是环烷基等；R2是（较低）烷氧基等；R3是（较低）烷基等；R4是（较低）烷基等；R5是羟基等；X是'0'，'S'，'SO'或'SO2'；Y是'CH'或'N'；n为0或1；或其药学上可接受的盐，可用作药物。
• Pyridine compounds, intermediates compositions and methods of use
  申请人：Eli Lilly and Company

  公开号：US05672609A1

  公开（公告）日：1997-09-30

  The present invention is directed to compounds of Formula I: ##STR1## wherein: n is 2 or 3; R is dimethylamino, diethylamino, 1-piperidinyl, 1-pyrrolidinyl, 4-morpholinyl, or 1-hexamethyleneimino; R.sup.1 is hydrogen, loweralkyl of C.sub.1 -C.sub.4, phenyl, or mono or di-substituted phenyl wherein each substituent is independently halo, methyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.6 -alkylsulfonyloxy; R.sup.2 is hydrogen, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.6 -alkylsulfonyloxy; and the pharmaceutically acceptable acid addition salts, which are for the treatment of post menopausal symptoms such as osteoporosis, cardiovascular conditions such as hyperlipidaemia, and the like.

  本发明涉及以下式I的化合物：其中：n为2或3；R为二甲基氨基，二乙基氨基，1-哌啶基，1-吡咯啉基，4-吗啉基，或1-己亚甲基氨基；R.sup.1为氢，C.sub.1-C.sub.4的低烷基，苯基，或单取代或双取代苯基，其中每个取代基独立地为卤素，甲基，羟基，C.sub.1-C.sub.6-烷氧基，苄氧基，C.sub.1-C.sub.6-烷酰氧基，苯甲酰氧基，取代苯甲酰氧基，带有1至3个取代基，每个取代基独立地为卤素，C.sub.1-C.sub.4-低烷基，或C.sub.1-C.sub.4-低烷氧基，C.sub.1-C.sub.5-烷氧羰氧基，或C.sub.4-C.sub.6-烷基磺酰氧基；R.sup.2为氢，羟基，C.sub.1-C.sub.6-烷氧基，苄氧基，C.sub.1-C.sub.6-烷酰氧基，苯甲酰氧基，取代苯甲酰氧基，带有1至3个取代基，每个取代基独立地为卤素，C.sub.1-C.sub.4-低烷基，或C.sub.1-C.sub.4-低烷氧基，C.sub.1-C.sub.5-烷氧羰氧基，或C.sub.4-C.sub.6-烷基磺酰氧基；以及药学上可接受的酸盐，用于治疗更年期后症状，如骨质疏松症，心血管疾病，如高脂血症等。
• Pyridine compounds intermediates processes compositions and methods
  申请人：Eli Lilly and Company

  公开号：US05750708A1

  公开（公告）日：1998-05-12

  The present invention is directed to compounds of Formula I: ##STR1## wherein: n is 2 or 3; R is dimethylamino, diethylamino, 1-piperidinyl, 1-pyrrolidinyl, 4-morpholinyl, or 1-hexamethyleneimino; R.sup.1 is hydrogen, loweralkyl of C.sub.1 -C.sub.4, phenyl, or mono or di-substituted phenyl wherein each substituent is independently halo, methyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.6 -alkylsulfonyloxy; R.sup.2 is hydrogen, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.6 -alkylsulfonyloxy; and the pharmaceutically acceptable acid addition salts, which are for the treatment of post menopausal symptoms such as osteoporosis, cardiovascular conditions such as hyperlipidaemia, and the like.

  本发明涉及式I的化合物：##STR1## 其中：n为2或3；R为二甲氨基，二乙氨基，1-哌啶基，1-吡咯基，4-吗啉基或1-己亚甲基亚胺基；R.sup.1为氢，C.sub.1-C.sub.4的低烷基，苯基或单取代或双取代苯基，其中每个取代基独立地为卤素，甲基，羟基，C.sub.1-C.sub.6-烷氧基，苄氧基，C.sub.1-C.sub.6-酰氧基，苯甲酰氧基，取代苯甲酰氧基，每个取代基独立地为卤素，C.sub.1-C.sub.4-低烷基或C.sub.1-C.sub.4-低烷氧基，C.sub.1-C.sub.5-烷氧羰氧基或C.sub.4-C.sub.6-烷基磺酰氧基；R.sup.2为氢，羟基，C.sub.1-C.sub.6-烷氧基，苄氧基，C.sub.1-C.sub.6-酰氧基，苯甲酰氧基，取代苯甲酰氧基，每个取代基独立地为卤素，C.sub.1-C.sub.4-低烷基或C.sub.1-C.sub.4-低烷氧基，C.sub.1-C.sub.5-烷氧羰氧基或C.sub.4-C.sub.6-烷基磺酰氧基；以及药学上可接受的酸盐，用于治疗绝经后症状，如骨质疏松症，心血管疾病，如高脂血症等。
• 1,2-disubstituted heterocyclic compounds
  申请人：EnVivo Pharmaceuticals, Inc.

  公开号：US08071595B2

  公开（公告）日：2011-12-06

  1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.

  本文描述了抑制磷酸二酯酶10的1,2-二取代杂环化合物。同时还描述了这些化合物的制备方法、制药组合物、制药制剂以及在哺乳动物（包括人类）治疗中枢神经系统（CNS）疾病和其他可能影响CNS功能的疾病中的制药用途。这些疾病包括但不限于与认知缺陷或精神分裂症状有关的神经学、神经退行性和精神障碍。