2-(4-Fluorobenzoyl)cyclohexanone | 2730-20-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(4-Fluorobenzoyl)cyclohexanone
• 英文别名: 2-(4-fluorobenzoyl)cyclohexan-1-one
• CAS: 2730-20-3
• 化学式: C₁₃H₁₃FO₂
• 分子量: 220.24
• InChiKey: YPFGOHKUMTXOKV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  34.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(4-Fluorobenzoyl)cyclohexanone 、 L-酪氨酸甲酯 以47.9的产率得到methyl 2-(2-(4-fluorobenzoyl)phenylamino)-3-(4-hydroxyphenyl)propionate
  参考文献：
  名称：

  [EN] SUBSTITUTED ARYLALCANOIC ACID DERIVATIVES AS PPAR PAN AGONISTS WITH POTENT ANTIHYPERGLYCEMIC AND ANTIHYPERLIPIDEMIC ACTIVITY
  [FR] DERIVES D'ACIDES ARYLALCANOIQUES SUBSTITUES SERVANT D'AGONISTES DE PPAR PAN AYANT UNE FORTE ACTIVITE ANTIHYPERGLYCEMIQUE ET ANTIHYPERLIPIDEMIQUE

  摘要：

  本发明涉及式I的取代芳基脂肪酸衍生物的制备和药物用途，其中环A、环B、R1、R2、R3、R4、R5、X、Alkl、Alk2、Arl和Ar2如规范中所定义。这些化合物作为选择性激动剂激活过氧化物酶体增殖物激活受体（PPAR），特别是RXR/PPARα，RXR/PPARγ和RXR/PPARδ异二聚体，在治疗和/或预防2型糖尿病和相关代谢综合征（如高血压、肥胖、胰岛素抵抗、高脂血症、高血糖、高胆固醇血症、动脉粥样硬化、冠状动脉疾病和其他心血管疾病）方面具有改善副作用剖面的功效，这些副作用通常与常规PPARγ激动剂有关。

  公开号：

  WO2004048333A1

文献信息

• Medicament for treating cerebral insufficiency diseases, novel
  申请人：Dainippon Pharmaceutical Co., Ltd.

  公开号：US05185338A1

  公开（公告）日：1993-02-09

  Medicament for the treatment of cerebral insufficiency diseases comprising as an active ingredient a compound of the formula: ##STR1## wherein n is 3, 4, 5 or 6; R.sup.1 is hydrogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, hydroxy-C.sub.2 -C.sub.6) alkyl, unsubstituted or substituted aryl, heteroaryl, unsubstituted or substituted aryl-(C.sub.1 -C.sub.6) alkyl, unsubstituted or substituted aryl-carbonyl-(C.sub.1 -C.sub.6) alkyl, or acyl; R.sup.2 is hydrogen atom, halogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, or trifluoromethyl; and R.sup.3 is hydrogen atom or C.sub.1 -C.sub.6 alkyl, or an acid addition salt thereof, novel 2-(1-piperazinyl)-4-phenyl-cycloalkanopyrimidine derivatives having excellent cerebral function improving activity, processes for the preparation thereof.

  治疗脑血管不足疾病的药物，其活性成分为公式为：##STR1## 其中n为3、4、5或6；R1为氢原子、C1-C6烷基、C3-C8环烷基、羟基-C2-C6)烷基、未取代或取代的芳基、杂环芳基、未取代或取代的芳基-(C1-C6)烷基、未取代或取代的芳基-羰基-(C1-C6)烷基或酰基；R2为氢原子、卤素原子、C1-C6烷基、C1-C6烷氧基或三氟甲基；R3为氢原子或C1-C6烷基，或其酸加成盐，新颖的2-(1-哌嗪基)-4-苯基-环烷基嘧啶衍生物具有优异的改善脑功能的活性，以及其制备方法。
• Substituted arylalcanoic acid derivatives as PPAR pan agonists with potent antihyperglycemic and antihyperlipidemic activity
  申请人：——

  公开号：US20040142921A1

  公开（公告）日：2004-07-22

  Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , R 5 , X, Alk 1 , Alk 2 , Ar 1 , and Ar 2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists. 1

  本发明涉及I式取代芳基脂肪酸衍生物的制备和药用，其中环A、环B、R1、R2、R3、R4、R5、X、Alk1、Alk2、Ar1和Ar2如规范中所定义。这些化合物作为选择性激动剂激活过氧化物酶体增殖物激活受体（PPAR），特别是RXR/PPARα、RXR/PPARγ和RXR/PPARδ异二聚体，在治疗和/或预防2型糖尿病和相关代谢综合征方面非常有用，例如高血压、肥胖、胰岛素抵抗、高脂血症、高血糖、高胆固醇血症、动脉粥样硬化、冠状动脉疾病和其他心血管疾病，且具有改善副作用剖面的优点，通常与传统的PPARγ激动剂有关。
• Substituted arylalcanoic acid derivatives as ppar pan agonists with potent antihyperglycemic and antihyperlipidemic activity
  申请人：Lu Xian-Ping

  公开号：US20080051321A1

  公开（公告）日：2008-02-28

  Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , R 5 , X, Alk 1 , Alk 2 , Ar 1 , and Ar 2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.

  本发明涉及一种Formula I的取代芳基脂肪酸衍生物的制备和药用，其中环A、环B、R1、R2、R3、R4、R5、X、Alk1、Alk2、Ar1和Ar2如规范中所定义。这些化合物作为选择性激动剂激活过氧化物酶体增殖物激活受体（PPAR），特别是RXR / PPARalpha，RXR / PPARgamma和RXR / PPARdelta异二聚体，在治疗和/或预防2型糖尿病和相关代谢综合症，如高血压、肥胖症、胰岛素抵抗、高脂血症、高血糖、高胆固醇血症、动脉粥样硬化、冠状动脉疾病和其他心血管疾病方面具有改善常见的PPARgamma激动剂副作用剖面。
• Medicament for treating cerebral insufficiency diseases containing 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof
  申请人：DAINIPPON PHARMACEUTICAL CO., LTD.

  公开号：EP0384228A1

  公开（公告）日：1990-08-29

  Medicament for the treatment of cerebral insufficiency diseases comprising as an active ingredient a compound of the formula: wherein n is 3, 4, 5 or 6; R¹ is hydrogen atom, C₁-C₆ alkyl, C₃-C₈ cycloalkyl, hydroxy-(C₂-C₆) alkyl, unsubstituted or substituted aryl, heteroaryl, unsubstituted or substituted aryl-(C₁-C₆) alkyl, unsubstituted or substituted aryl­carbonyl-(C₁-C₆) alkyl, or acyl; R² is hydrogen atom, halogen atom, C₁-C₆ alkyl, C₁-C₆ alkoxy, or trifluoromethyl; and R³ is hydrogen atom or C₁-C₆ alkyl, or an acid addition salt thereof, novel 2-(1-piperazinyl)-4-phenyl-cycloalkano­pyrimidine derivatives having excellent cerebral function improving activity, processes for the preparation thereof.

  用于治疗脑功能不全疾病的药物，其有效成分包括以下式子的化合物 其中 n 为 3、4、5 或 6；R¹ 是氢原子、C₁-C₆ 烷基、C₃-C₈ 环烷基、羟基-(C₂-C₆) 烷基、未取代或取代的芳基、杂芳基、未取代或取代的芳基-(C₁-C₆) 烷基、未取代或取代的芳羰基-(C₁-C₆) 烷基或酰基；R²是氢原子、卤素原子、C₁-C₆烷基、C₁-C₆烷氧基或三氟甲基；以及 R³是氢原子或 C₁-C₆烷基，或其酸加成盐，新型 2-(1-哌嗪基)-4-苯基环烷基嘧啶衍生物具有优异的改善脑功能活性，及其制备工艺。
• 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives and pharmaceutical composition containing the same
  申请人：DAINIPPON PHARMACEUTICAL CO., LTD.

  公开号：EP0484988A1

  公开（公告）日：1992-05-13

  Novel 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives of the formula: wherein n is 3, 5 or 6, or a pharmaceutically acceptable acid addition salt thereof, which is useful for the treatment of the cerebral insufficiency diseases.

  新型 2-(1-哌嗪基)-4-苯基环烷嘧啶衍生物（式中 n 为 3、5 或 6）或其药学上可接受的酸加成盐，可用于治疗脑功能不全疾病。