p-Fluorbenzoyl-4-piperidinopropanol | 25503-64-4

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: p-Fluorbenzoyl-4-piperidinopropanol
• 英文别名: 4-(p-Fluorbenzoyl)-1-(3-hydroxypropyl)-piperidin；4-(4-Fluorobenzoyl)-1-(3-hydroxypropyl)piperidine；4-(p-fluorobenzoyl)-1-(3-hydroxypropyl)piperidine；(4-fluoro-phenyl)-[1-(3-hydroxy-propyl)-piperidin-4-yl]-methanone；(4-fluorophenyl)-[1-(3-hydroxypropyl)piperidin-4-yl]methanone
• CAS: 25503-64-4
• 化学式: C₁₅H₂₀FNO₂
• 分子量: 265.328
• InChiKey: AKXHPNYPANDETL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  p-Fluorbenzoyl-4-piperidinopropanol 在 sodium hydroxide 、 氯化亚砜 作用下， 以 氯仿 为溶剂， 生成 1-(γ-chloropropyl)-4-(4-fluorobenzoyl)piperidine
  参考文献：
  名称：

  1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones

  摘要：

  式##STR1##所示的1,5-二取代-1,2-二氢-2H-1,4-苯并二氮杂卓-2-酮，其中R为氢或氟，R1为氢、氟、氯、溴或三氟甲基，且n为2至4，具有抗惊厥活性并可用作抗焦虑剂，已被公开。

  公开号：

  US04151285A1
• 作为产物：
  描述：

  4-(4-氟苯甲酰基)哌啶 、 异丙醚 、 3-溴-1-丙醇 在 potassium carbonate 作用下， 以 异丙醇 、 正丁醇 为溶剂， 生成 p-Fluorbenzoyl-4-piperidinopropanol
  参考文献：
  名称：

  1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones

  摘要：

  式##STR1##所示的1,5-二取代-1,2-二氢-2H-1,4-苯并二氮杂卓-2-酮，其中R为氢或氟，R1为氢、氟、氯、溴或三氟甲基，且n为2至4，具有抗惊厥活性并可用作抗焦虑剂，已被公开。

  公开号：

  US04151285A1

文献信息

• Syntheses of 5-HT2 antagonist activity of bicyclic 1,2,4-triazol-3(2H)-one and 1,3,5-triazine-2,4(3H)-dione derivatives
  作者：Yoshifumi Watanabe、Hiroyuki Usui、Shozo Kobayashi、Hirotaka Yoshiwara、Toshiro Shibano、Tsuyoshi Tanaka、Yoshiyuki Morishima、Megumi Yasuoka、Munefumi Kanao

  DOI：10.1021/jm00079a026

  日期：1992.1

  2,4-triazol-3(2H)-one and 1,3,5-triazine-2,4(3H)-dione derivatives with a 4-[bis(4-fluoro-phenyl)methylene]piperidine or 4-(4-fluorobenzoyl)piperidine group has been prepared and tested for 5-HT2 and alpha 1 receptor antagonist activity. Among the compounds prepared, 2-[2-[4-[bis(4-fluorophenyl)methylene]-piperidin-1-yl]ethyl]- 5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyridin-3(2H)-one (7b) had the most

  一系列带有4- [双（4-氟-苯基）亚甲基的双环1,2,4-三唑-3（2H）-one和1,3,5-三嗪-2,4（3H）-二酮衍生物已制备]哌啶或4-（4-氟苯甲酰基）哌啶基团并测试了5-HT 2和α1受体拮抗剂的活性。在制备的化合物中，2- [2- [2- [4- [双（4-氟苯基）亚甲基]-哌啶-1-基]乙基] -5,6,7,8-四氢-1,2,4-三唑[ 4,3-a] pyridin-3（2H）-one（7b）具有最有效的5-HT2拮抗剂活性，高于利坦色林（2），而7b在体内未显示出α1拮抗剂活性。当测试阻断5-羟色氨酸诱导的头部抽搐的能力时，中央5-HT 2受体拮抗作用约为2的1/30。化合物21b，3- [2- [4-（4-氟苯甲酰基）哌啶-1-基]乙基] -6,7,8,9-四氢-2H-吡啶基[1,2-a] -1,3， 5-三嗪-2，4（3H）-二酮也显示出有效的5-HT2拮抗剂活性
• Syntheses of monocyclic and bicyclic 2,4(1H,3H)-pyrimidinediones and their serotonin 2 antagonist activities.
  作者：Yoshifumi WATANABE、Hiroyuki USUI、Toshiro SHIBANO、Tsuyoshi TANAKA、Munefumi KANAO

  DOI：10.1248/cpb.38.2726

  日期：——

  New serotonine 2(5-HT2) antagonists with a monocyclic or bicyclic 2, 4(1H, 3H)-pyrimidinedione have been prepared and their activities evaluated. In a series of monocyclic compounds, 1-substituted 5-phenyl-2, 4(1H, 3H)-pyrimidinedione 14 showed potent in vitro activity, and the corresponding 3-substituted 5-phenyl and 6-phenyl derivatives 3, 8 and 20a also showed moderate activity. In the bicyclic compounds, 3-substituted 5, 6, 7, 8-tetrahydro-2, 4(1H, 3H)-quinazolinedione 33 exhibited the most potent activity among the compounds prepared in this paper. The in vivo antagonist activity of 33 was comparable of that of ketanserin, a typical peripheral 5-HT2 antagonist.

  新型血清素2(5-HT2)拮抗剂已通过单环或双环2, 4(1H, 3H)-嘧啶二酮的合成制备，并评估了其活性。在一系列单环化合物中，1-取代的5-苯基-2, 4(1H, 3H)-嘧啶二酮14显示出强的体外活性，而相应的3-取代的5-苯基和6-苯基衍生物3、8和20a也表现出中等活性。在双环化合物中，3-取代的5, 6, 7, 8-四氢-2, 4(1H, 3H)-喹唑啉二酮33在本文中制备的化合物中表现出最强的活性。化合物33的体内拮抗活性与酮哌齐（典型的周围5-HT2拮抗剂）相当。
• Subtype-selective NMDA receptor ligands and the use thereof
  申请人：——

  公开号：US20010051633A1

  公开（公告）日：2001-12-13

  The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

  本发明涉及亚型选择性NMDA受体配体及其用于治疗或预防与中风、缺血、中枢神经系统创伤、低血糖和手术相关的神经元丧失，以及治疗包括阿尔茨海默病、肌萎缩性侧索硬化症、亨廷顿病和唐氏综合症在内的神经退行性疾病，治疗或预防兴奋性氨基酸过度刺激的不良后果，治疗焦虑，精神病，惊厥，氨基糖苷类抗生素引起的听力损失，偏头痛，慢性疼痛，帕金森病，青光眼，巨细胞病毒性视网膜炎，尿失禁，阿片类耐受或戒断，并诱导麻醉，以及增强认知能力。
• 10-[.omega.-(BENZOYLPIPERIDINYL)ALKYL]PHENOTHIAZINES
  申请人：A. H. Robins Company, Incorporated

  公开号：US04021552A1

  公开（公告）日：1977-05-03

  10-[.omega.-(Benzoylpiperidinyl)alkyl]phenothiazines having the formula ##STR1## wherein R is hydrogen, chloro, bromo, trifluoromethyl, lower alkoxy, acetyl, sulfamoyl, or dimethylsulfamoyl, R.sup.1 is hydrogen, chloro, bromo, fluoro, trifluoromethyl, lower alkyl or lower alkoxy and n is 2, 3 or 4 are disclosed. Methods for the preparation of the compounds are described. The compounds possess tranquilizing activity and are useful as tranquilizing agents in mammals.

  公开了具有以下式子的10-[.omega.-(苯甲酰基哌啶基)烷基]苯并噻嗪：##STR1##其中R为氢，氯，溴，三氟甲基，低烷氧基，乙酰基，磺酰氨基或二甲基磺酰氨基，R.sup.1为氢，氯，溴，氟，三氟甲基，低烷基或低烷氧基，n为2、3或4。描述了制备这些化合物的方法。这些化合物具有镇静作用，可用作哺乳动物的镇静剂。
• Heterocyclic compound having serotonine 2-receptor antagonistic activity
  申请人：Daiichi Pharmaceutical Co., Ltd.

  公开号：US05232924A1

  公开（公告）日：1993-08-03

  A heterocyclic compound represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group, an aryl group which may be substituted with one or more substituents selected from the group consisting of a halogen atom, an alkoxy group, an alkyl group and a trihalogenomethyl group; .lambda. represents 0 or 1; ring A represents a 6 membered heterocyclic ring containing the nitrogen atom shared with the triazine ring and which may contain one or more double bonds; Y represents a substituted or unsubstituted alkylene group having 1 to 15 carbon atoms; and Q represents a group represented by formula (II): ##STR2## wherein R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are represented by substituents disclosed herein; or salt thereof, and intermediates therefor are described. The compound of formula (I) or salt thereof exhibit selective serotonin 2-receptor antagonistic activity and are useful for the prevention or treatment of circulatory diseases, e.g., ischemic heart diseases, cerebral vessel disturbances, and peripheral circulation disturbances.

  一种由式（I）表示的杂环化合物：##STR1## 其中R.sup.1表示氢原子，烷基，芳基，可以用来替代一个或多个取代基的芳基，所述取代基选择自卤原子，烷氧基，烷基和三卤甲基；λ表示0或1；环A表示一个含有与三嗪环共享的氮原子的6元杂环环，该环可以包含一个或多个双键；Y表示取代或未取代的碳数为1至15的烷基；Q表示由式（II）表示的基团：##STR2## 其中R.sup.2，R.sup.3，R.sup.4和R.sup.5由此处披露的取代基团表示；或其盐和中间体。式（I）或其盐具有选择性5-羟色胺2受体拮抗活性，并且对于预防或治疗循环系统疾病，例如缺血性心脏病，脑血管障碍和周围循环障碍是有用的。