2-(5-fluoro-2-methoxyphenoxy)-ethanol | 72955-98-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-(5-fluoro-2-methoxyphenoxy)-ethanol
• 英文别名: 2-(5-Fluoro-2-methoxyphenoxy)ethanol
• CAS: 72955-98-7
• 化学式: C₉H₁₁FO₃
• 分子量: 186.183
• InChiKey: LJFLKLZPTIKGGE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  38.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  5-氟-2-甲氧基苯酚 以89%的产率得到2-(5-fluoro-2-methoxyphenoxy)-ethanol
  参考文献：
  名称：

  Certain aryl-aliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases

  摘要：

  通式（I）的化合物： 其中变量如规范中定义的那样，对于预防或治疗人类或动物中与血清素相关，特别是5-HT2受体相关的疾病是有用的，特别是与5-HT2c受体相关的疾病，尤其是与进食障碍、记忆障碍、精神分裂症、情绪障碍、焦虑障碍、疼痛、性功能障碍和尿液障碍等疾病相关的疾病。

  公开号：

  US06465467B1

文献信息

• Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions
  申请人：Boehringer Mannheim GmbH

  公开号：US04503067A1

  公开（公告）日：1985-03-05

  Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl; R.sub.2 is hydrogen, lower alkyl or arylalkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen or lower alkyl, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--; X is a valency bond, --CH.sub.2 --, oxygen or sulfur; Ar is mono- or bicyclic aryl or pyridyl; R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl; R.sub.5 and R.sub.6 together can represent methylenedioxy; and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.

  Carbazolyl-(4)-oxypropanolamine化合物的化学式为##STR1##其中R.sub.1是氢，较低的烷酰基或芳酰基；R.sub.2是氢，较低的烷基或芳基烷基；R.sub.3是氢或较低的烷基；R.sub.4是氢或较低的烷基，或者当X是氧时，R.sub.4与R.sub.5一起可以代表--CH.sub.2--O--；X是一个价键，--CH.sub.2--，氧或硫；Ar是单环或双环芳基或吡啶基；R.sub.5和R.sub.6分别选自氢，卤素，羟基，较低的烷基，氨基甲酰基，较低的烷氧基，芳基烷氧基，较低的烷基硫基，较低的烷基磺基；R.sub.5和R.sub.6一起可以代表亚甲二氧基；以及它们与生理上可接受的酸盐在治疗和预防循环和心脏疾病，例如高血压和心绞痛方面具有卓越的疗效。
• Phenoxyethylamine derivatives, for preparing the same and composition
  申请人：Hokuriku Pharmaceutical Co., Ltd.

  公开号：US04971990A1

  公开（公告）日：1990-11-20

  Phenoxyethylamine derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 and R.sub.5 represent lower-alkyl, R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen or lower-alkyl, or ##STR2## represents a 5- or 6-membered ring system which may include nitrogen, oxygen or sulfur as a ring membered atom, R.sub.4 represents hydrogen or lower-alkyl, and n represents an integer selected from 1 to 3, their optical isomers and pharmacologically-acceptable acid addition salts, which exhibit excellent .alpha..sub.1 -blocking activity, a process for their preparation, pharmaceutical compositions thereof, and a method for the treatment of a subject afflicted with hypertension or dysuria by administrating such a compound, are all disclosed.

  本发明揭示了一种由通式（I）表示的苯氧乙胺衍生物：##STR1## 其中R.sub.1和R.sub.5表示较低的烷基，R.sub.2和R.sub.3，可以相同或不同，每个表示氢或较低的烷基，或##STR2##表示一个5-或6-成员环系，其中可以包括氮、氧或硫作为环成员原子，R.sub.4表示氢或较低的烷基，n表示选择从1到3的整数，其光学异构体和药理学上可接受的酸加盐，表现出优异的α.sub.1-阻断活性，其制备方法，制药组合物以及通过管理此类化合物治疗患有高血压或排尿困难的受试者的方法。
• CERTAIN ARYLALIPHATIC AND HETEROARYL-ALIPHATIC PIPERAZINYL PYRAZINES AND THEIR USE IN THE TREATMENT OF SEROTONIN-RELATED DISEASES
  申请人：Biovitrum, AB, a Stockholm, Sweden corporation

  公开号：US20040242554A1

  公开（公告）日：2004-12-02

  The invention relates to compounds of the general formula (I): 1 wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO 2 —, —NH—, (ii) a C 1-4 -alkyl- or C 1-6 -acyl-substituted nitrogen atom or (iii) a C 1-8 -alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R 4 )(R 5 )—, —OC(R 4 )(R 5 )—, —N(R 6 )C(R 4 )(R 5 )—, —N(R 6 )—, —O—, —S— or —SO 2 —; R is optionally substituted C 3-8 -cycloalkyl, aryl or heteroaryl; R 1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R 4 )(R 5 )] x N(R 2a )(R 3a )]; R 2a , R 3a , R 4 , R 5 , R 6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory, disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).

  本发明涉及通式（I）的化合物：其中Ar是可选取代的芳基或杂芳基；A是（i）—O—，—S—，—SO2—，—NH—，（ii）C1-4烷基或C1-6酰基取代的氮原子，或（iii）C1-8烷基链或具有2-8链原子的杂烷基链，其可选包含至少一个不饱和度，并且可以取代和/或含有桥接以形成具有3-8环成员的饱和或部分或完全不饱和环；B是—C（R4）（R5）—，—OC（R4）（R5）—，—N（R6）C（R4）（R5）—，—N（R6）—，—O—，—S—或—SO2—；R是可选取代的C3-8环烷基，芳基或杂芳基；R1是（i）饱和或不饱和的氮杂环或氨基氮杂环，或饱和的二氮杂环或氨基二氮杂环，其具有4-7环成员，或饱和的氨基氮杂双环、氮杂双环或二氮杂双环，其具有7-10环成员，这些环在一个或多个位置上可选取代，或者是一个组—[C（R4）（R5）]xN（R2a）（R3a）；R2a，R3a，R4，R5，R6和x如权利要求中所定义，n为0或1；以及其药学上可接受的盐、水合物和前药形式。这些化合物可以通过常规方法制备，并可用于治疗患有血清素相关疾病的人或动物，例如进食障碍，尤其是肥胖症，记忆障碍，精神分裂症，情绪障碍，焦虑障碍，疼痛，性功能障碍和泌尿系统疾病。本发明还涉及这种用途以及包含通式（I）化合物的制药组合物。
• Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
  申请人：Biovitrum, AB, a Stockholm, Sweden corporation

  公开号：US20030092694A1

  公开（公告）日：2003-05-15

  The invention relates to compounds of the general formula (I): 1 wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO 2 —, —NH—, (ii) a C 1-4 -alkyl- or C 1-6 -acyl-substituted nitrogen atom or (iii) a C 1-8 -alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R 4 )(R 5 )—, —OC(R 4 )(R 5 )—, —N(R 6 )C(R 4 )(R 5 )—, —N(R 6 )—, —O—, —S— or —SO 2 —; R is optionally substituted C 3-8 -cycloalkyl, aryl or heteroaryl; R 1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R 4 )(R 5 )] x N(R 2a )(R 3a )]; R 2a , R 3a , R 4 , R 5 , R 6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I)

  本发明涉及一般式（I）的化合物：其中Ar是可选取代的芳基或杂环芳基；A是（i）-O-，-S-，-SO2-，-NH-，（ii）C1-4-烷基或C1-6-酰基取代的氮原子或（iii）C1-8-烷基链或具有2至8个链原子的杂烷基链，可选地含有至少一个不饱和度，并且可以取代和/或包含桥以形成具有3-8个环成员的饱和或部分或完全不饱和的环；B是-C（R4）（R5）-，-OC（R4）（R5）-，-N（R6）C（R4）（R5）-，-N（R6）-，-O-，-S-或-SO2-；R是可选取代的C3-8-环烷基，芳基或杂环芳基；R1是（i）饱和或不饱和的氮杂环或氨基氮杂环环，或具有4至7个环成员的饱和二氮杂环或氨基二氮杂环环，或具有7至10个环成员的饱和氨基氮杂双环、氮杂双环或二氮杂双环环，这些环可选地在一个或多个位置上取代，或一个组-［C（R4）（R5）］xN（R2a）（R3a）；其中R2a，R3a，R4，R5，R6和x如所述，n为0或1；以及其药学上可接受的盐、水合物和前药形式。这些化合物可以通过常规方法制备，并可用于治疗患有血清素相关疾病的人类或动物受试者，例如进食障碍，特别是肥胖，记忆障碍，精神分裂症，情绪障碍，焦虑症，疼痛，性功能障碍和泌尿系统疾病。本发明还涉及这种用途以及包含式（I）化合物的药物组合物。
• Phenoxyethylamine derivatives, process for preparing the same, and composition for exhibiting excellent alpha-1-blocking activity containing the same
  申请人：Hokuriku Pharmaceutical Co.,Ltd

  公开号：EP0331943A1

  公开（公告）日：1989-09-13

  Phenoxyethylamine derivatives represented by the general formula (I): wherein R₁ and R₅ represent lower-alkyl, R₂ and R₃, which may be the same or different, each represents hydrogen or lower-alkyl, or represents a 5- or 6-membered ring system which may include nitrogen, oxygen or sulfur as a ring membered atom, R₄ represents hydrogen or lower-alkyl, and n represents an integer selected from 1 to 3, their optical isomers and pharmacologically-acceptable acid addition salts, which exhibit excellent α₁-blocking activity, a process for their preparation, pharmaceutical compositions thereof, and a method for the treatment of a subject afflicted with hypertension or dysuria by administrating such a compound, are all disclosed.

  通式(I)代表的苯氧基乙胺衍生物： 其中 R₁ 和 R₅ 代表低级烷基，R₂ 和 R₃ 可以相同或不同，各自代表氢或低级烷基，或 代表可包括氮、氧或硫作为环成员原子的 5 或 6 元环系统，R₄ 代表氢或低级烷基，n 代表选自 1 至 3 的整数，它们的光学异构体和药理学上可接受的酸加成盐、本发明公开了具有优异α₁阻断活性的光学异构体和药理学上可接受的酸加成盐、其制备工艺、药物组合物，以及通过施用这种化合物治疗高血压或排尿困难患者的方法。