1-(3-Fluoro-4-methoxyphenyl)-2-(4-methoxyphenyl)ethanone | 225668-40-6

• 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-(3-Fluoro-4-methoxyphenyl)-2-(4-methoxyphenyl)ethanone
• 英文别名: 3'-fluoro-4'-methoxy-2-(4-methoxyphenyl)acetophenone；1-(3-Fluoro-4-methoxy-phenyl)-2-(4-methoxy-phenyl)-ethanone
• CAS: 225668-40-6
• 化学式: C₁₆H₁₅FO₃
• 分子量: 274.292
• InChiKey: MZZMSNXSGCFXKA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(3-Fluoro-4-methoxyphenyl)-2-(4-methoxyphenyl)ethanone 、 酒石酸 在 sodium periodate 、 硫酸 、 sodium hydroxide 作用下， 以 水 、 乙醇 为溶剂， 反应 0.5h， 生成 3,4-bis(4-methoxyphenyl)-2-hydroxy-4-oxobutanoic acid
  参考文献：
  名称：

  Pyridazine compounds and compositions containing the same

  摘要：

  这项发明涉及由式（1）表示的吡啶嗪衍生物： 其中R1代表（取代的）芳基，R2代表在4位被低烷氧基或低烷硫基取代的苯基，R3代表低烷氧基、卤代低烷基、低环烷基、（取代的）芳基、（取代的）芳氧基、（取代的）含氮杂环环残基、（取代的）氨基羰基或低烷基羰基，A代表单键、低烷基烯基或低烷烯基，X代表O或S，虚线表示4位和5位之间的碳-碳键为单键或双键，或其盐；以及含有它们作为有效成分的药物。这些化合物对白细胞介素-1β的产生具有出色的抑制活性，并可用作免疫系统疾病、炎症性疾病、缺血性疾病等的预防和治疗药物。

  公开号：

  US06348468B1
• 作为产物：
  描述：

  2-氟苯甲醚 、 4-甲氧基苯乙酰氯 在 aluminum (III) chloride 作用下， 以 二氯甲烷 为溶剂， 反应 2.5h， 以49.6%的产率得到1-(3-Fluoro-4-methoxyphenyl)-2-(4-methoxyphenyl)ethanone
  参考文献：
  名称：

  Pyridazine compounds and compositions containing the same

  摘要：

  这项发明涉及由式（1）表示的吡啶嗪衍生物： 其中R1代表（取代的）芳基，R2代表在4位被低烷氧基或低烷硫基取代的苯基，R3代表低烷氧基、卤代低烷基、低环烷基、（取代的）芳基、（取代的）芳氧基、（取代的）含氮杂环环残基、（取代的）氨基羰基或低烷基羰基，A代表单键、低烷基烯基或低烷烯基，X代表O或S，虚线表示4位和5位之间的碳-碳键为单键或双键，或其盐；以及含有它们作为有效成分的药物。这些化合物对白细胞介素-1β的产生具有出色的抑制活性，并可用作免疫系统疾病、炎症性疾病、缺血性疾病等的预防和治疗药物。

  公开号：

  US06348468B1

文献信息

• TETRAHYDRONAPHTHALEN-2-OL DERIVATIVES
  申请人：Stock Herman Thijs

  公开号：US20100240748A1

  公开（公告）日：2010-09-23

  The present invention relates to novel tetrahydronaphthalen-2-ol derivatives, to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the manufacture of a medicament for the prevention or treatment of lower urinary tract symptoms, benign prostate hyperplasia, prostate cancer, hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer.

  本发明涉及新型四氢萘-2-醇衍生物，包括这些化合物的药物组合物以及它们在治疗中的应用，特别是它们用于制造预防或治疗下尿道症状、良性前列腺增生、前列腺癌、潮热、焦虑、抑郁、乳腺癌、髓样甲状腺癌、卵巢癌、炎症性肠病、关节炎、子宫内膜异位症和结肠癌的药物的用途。
• [EN] TETRAHYDRONAPHTHALEN-2-OL DERIVATIVES<br/>[FR] DÉRIVÉS DU TÉTRAHYDRONAPHTALÈN-2-OL
  申请人：ORGANON NV

  公开号：WO2010103095A1

  公开（公告）日：2010-09-16

  The present invention relates to novel tetrahydronaphthalen-2-ol derivatives, to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the manufacture of a medicament for the prevention or treatment of lower urinary tract symptoms,benign prostate hyperplasia,prostate cancer,hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer.

  本发明涉及新型四氢萘-2-醇衍生物，包括这些化合物的药物组合物，以及它们在治疗中的应用，特别是用于制造用于预防或治疗下尿路症状、良性前列腺增生、前列腺癌、潮热、焦虑、抑郁、乳腺癌、髓样甲状腺癌、卵巢癌、炎症性肠病、关节炎、子宫内膜异位症和结肠癌的药物。
• Novel pyridazine derivatives and medicines containing the same as effective ingredients
  申请人：Ohkuchi Masao

  公开号：US20050267113A1

  公开（公告）日：2005-12-01

  This invention relates to pyridazine derivatives represented by the formula (1): wherein R 1 represents a (substituted) aryl group, R 2 represents a phenyl group substituted at 4 -position by a lower alkoxyl group or a lower alkylthio group, R 3 represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (subsituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4 -position and the 5 -position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin- 1 β production, and are useful as preventives and therapeutics for immmune system diseases, inflammatory diseases, ischemic diseases and the like.

  本发明涉及由式（1）表示的吡嗪衍生物：其中R1表示（取代）芳基基团，R2表示在4-位被低烷氧基基团或低烷硫基基团取代的苯基基团，R3表示低烷氧基基团、卤代低烷基基团、低环烷基基团、（取代）芳基基团、（取代）芳氧基基团、（取代）含氮杂环环残基、（取代）氨基甲酰基或低烷基甲酰基，A表示单键、低烷基亚ethylene基或低烷基亚烯基，X表示O或S，虚线表示4-位和5-位之间的碳-碳键为单键或双键，或其盐；以及包含它们作为有效成分的药物。这些化合物对白细胞介素-1β的产生有出色的抑制活性，并且可用作免疫系统疾病、炎症性疾病、缺血性疾病等的预防和治疗。
• NOVEL PYRIDAZINE DERIVATIVES AND MEDICINES CONTAINING THE SAME AS EFFECTIVE INGREDIENTS
  申请人：OHKUCHI Masao

  公开号：US20090270399A1

  公开（公告）日：2009-10-29

  This invention relates to pyridazine derivatives represented by the formula (1): wherein R 1 represents a (substituted) aryl group, R 2 represents a phenyl group substituted at 4-position by a lower alkoxyl, group or a lower alkylthio group, R 3 represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (substituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1β production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.

  本发明涉及由式（1）表示的吡嗪衍生物： 其中R1表示（取代的）芳基基团，R2表示在4位被低烷氧基团或低烷硫基团取代的苯基基团，R3表示低烷氧基团、卤代的低烷基团、低环烷基团、（取代的）芳基基团、（取代的）芳氧基基团、（取代的）含氮杂环环残基、（取代的）氨基甲酰基团或低烷基甲酰基团，A表示单键、低烷基烷基或低烯基烷基，X表示O或S，虚线表示4位和5位之间的碳-碳键为单键或双键，或其盐；以及含有它们作为有效成分的药物。这些化合物具有优异的抑制白细胞介素-1β产生的活性，可用作预防和治疗免疫系统疾病、炎症性疾病、缺血性疾病等。
• NOVEL PYRIDAZINE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
  申请人：Kowa Co., Ltd.

  公开号：EP1043317A1

  公开（公告）日：2000-10-11

  This invention relates to pyridazine derivatives represented by the formula (1): wherein R1 represents a (substituted) aryl group, R2 represents a phenyl group substituted at 4-position by a lower alkoxyl group or a lower alkylthio group, R3 represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (subsituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1β production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.

  本发明涉及式（1）所代表的哒嗪衍生物： 其中 R1 代表（取代的）芳基，R2 代表在 4 位被低级烷氧基或低级烷硫基取代的苯基，R3 代表低级烷氧基、卤代低级烷基、低级环烷基、（取代的）芳基、（取代的）芳氧基、（取代的）含氮杂环残基、一个（取代的）氨基羰基或一个低级烷基羰基，A 代表单键、一个低级亚烷基或一个低级亚烯基，X 代表 O 或 S，虚线表示 4 位和 5 位之间的碳-碳键是单键或双键，或其盐；以及含有这些化合物作为有效成分的药物。这些化合物对白细胞介素-1β的产生具有良好的抑制活性，可作为免疫系统疾病、炎症性疾病、缺血性疾病等的预防和治疗药物。