2-(3-Methylpiperidin-2-yl)ethan-1-ol | 30364-12-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 2-(3-Methylpiperidin-2-yl)ethan-1-ol
• 英文别名: 2-(3-methylpiperidin-2-yl)ethanol
• CAS: 30364-12-6
• 化学式: C₈H₁₇NO
• mdl: MFCD19225794
• 分子量: 143.229
• InChiKey: JNHKCGCZVXJPGT-UHFFFAOYSA-N

物化性质

• 沸点：
  242.4±13.0 °C(Predicted)
• 密度：
  0.909±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(3-Methylpiperidin-2-yl)ethan-1-ol 在 苯甲醚 、 三苯基膦 、 三氟乙酸 、 偶氮二甲酸二乙酯 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 19.0h， 生成 7-Chloro-3-(3,5-dimethyl-phenyl)-4-[2-(3-methyl-piperidin-2-yl)-ethoxy]-6-nitro-1H-quinolin-2-one
  参考文献：
  名称：

  Syntheses and structure–activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists

  摘要：

  Syntheses and structure-activity relationships of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists are described. Some of substituents on the piperidine ring that were investigated included a fused phenyl group, a (6R)-trifluoromethyl group, (6S) and (6R)-methyl group. This study showed that GnRH binding potency was tolerated by a small group at the 6-position of the piperidine, and blocking the 6-position by a trifluoromethyl group reduced clearance rate and increased oral bioavailability. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2003.12.101
• 作为产物：
  描述：

  ethyl 3-methyl-2-pyridineacetate 在 platinum(IV) oxide 氢气 、 溶剂黄146 作用下， 20.0 ℃ 、310.26 kPa 条件下， 反应 12.0h， 生成 2-(3-Methylpiperidin-2-yl)ethan-1-ol
  参考文献：
  名称：

  Syntheses and structure–activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists

  摘要：

  Syntheses and structure-activity relationships of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists are described. Some of substituents on the piperidine ring that were investigated included a fused phenyl group, a (6R)-trifluoromethyl group, (6S) and (6R)-methyl group. This study showed that GnRH binding potency was tolerated by a small group at the 6-position of the piperidine, and blocking the 6-position by a trifluoromethyl group reduced clearance rate and increased oral bioavailability. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2003.12.101

文献信息

• Pyrazolopyridine compound and processes for preparation thereof
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0299209A2

  公开（公告）日：1989-01-18

  A pyrazolopyridine compound of the formula : wherein R1 is lower alkyl, aryl which may have one or more suitable substituent(s) or a heterocyclic group, R2 is a group of the formula: (wherein R4 is protected amino or hydroxy and R5 is hydrogen or lower alkyl) ; cyano; a group of the formula: -A-R6 (wherein R6 is an acyl group, and A is lower aliphatic hydrocarbon group which may have one or more suitable substituent(s)); amidated carboxy; amino or protected amino; and R3 is hydrogen, lower alkyl, lower alkoxy or halogen and a pharmaceutically acceptable salt thereof, processes for their preparation and pharmaceutical compositions comprising them.

  式中的吡唑并吡啶化合物： 其中 R1 是低级烷基、可具有一个或多个合适取代基的芳基或杂环基团，R2 是式中的基团： (其中 R4 是受保护的氨基或羟基，R5 是氢或低级烷基）； 氰基 式中的基团 -A-R6 (其中 R6 是酰基，A 是低级脂肪族烃基，可具有一个或多个合适的取代基）；酰胺化羧基；氨基或受保护氨基；以及 R3 是氢、低级烷基、低级烷氧基或卤素及其药学上可接受的盐、它们的制备工艺和包含它们的药物组合物。
• NOVEL USE OF PYRAZOLOPYRIDINE COMPOUNDS
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0823254A1

  公开（公告）日：1998-02-11

  The present invention relates to a pharmaceutical composition for the prevention and/or the treatment of dialysis-induced hypotension and/or hypotension after dialysis which comprises, as an active ingredient, a pyrazolopyridine compound of the following formula : wherein R1 islower alkyl, etc, R2 isa group of the formula : (wherein R4 isprotected amino, etc and R5 ishydrogen, etc); etc, and R3 ishydrogen, etc, or a salt thereof.

  本发明涉及一种用于预防和/或治疗透析引起的低血压和/或透析后低血压的药物组合物，其活性成分包括下式的吡唑并吡啶化合物： 其中 R1 是低级烷基等 R2 为下式基团 其中 R4 是受保护的氨基等，以及 R5 是氢等）；等，以及 R3 是氢等、 或其盐。
• PREVENTIVES AND REMEDIES FOR ISCHEMIC INTESTINAL LESION AND ILEUS
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0900796A1

  公开（公告）日：1999-03-10

  The present invention relates to a prophylactic and/or therapeutic composition for ischemic intestinal lesions and/or ileus which comprises as an active ingredient a pyrazolopyridine compound of the following formula: [wherein R1 is lower alkyl group, etc; R2 is a group of the formula: (wherein R4 is protected amino group, etc; R5 is hydrogen, etc);etc, and R3 is hydrogen, etc] or a salt thereof.

  本发明涉及一种用于缺血性肠病变和/或回肠炎的预防性和/或治疗性组合物，其活性成分包括下式的吡唑并吡啶化合物： [其中 R1 是低级烷基等；R2 是式中的基团： (其中 R4 为受保护的氨基等；R5 为氢等）；等，以及 R3 为氢等]或其盐。
• 1,2-Di-substituted piperidine derivatives as hair growth promoter
  申请人：SHISEIDO COMPANY LIMITED

  公开号：EP0933361A1

  公开（公告）日：1999-08-04

  A 1,2-di-substituted piperidine derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C1-30 expressed by R1 and the other is -(CH2)n-NR2R3; Y is -CO-, -CONR5- or -COO-; Z is -O-, -OCO-, -OCONR6- or -NR6-; R2 and R3 individually represent a hydrogen a lower alkyl, a phenyl or a benzyl group, or together represent a heterocycle having 3-7 members; -NR5-(CH2)n-NR2R3 and -NR6-(CH2)n-NR2R3 of -(Y)1-A and -Z-B may be the following Group W: wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R2 is a hydrogen, a lower alkyl, a phenyl or a benzyl group; R4 is a hydrogen, a halogen, a lower alkyl, a lower acyl, a nitro, a cyano, a lower alkoxycarbonyl, a carbamoyl, a lower alkylcarbamoyl, a lower alkylamino, a lower acylamino, a lower alkoxy or a lower acyloxy group; each of R5 and R6 is a hydrogen, a lower alkyl, a lower acyl, a lower alkylcarbamoyl group, or a part of said ring E; l is 0 or 1; m is an integer of 2-5; and n is an integer of 0-5. The 1,2-di-substituted piperidine derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.

  一种 1,2-二取代的哌啶衍生物或其盐，由下式（I）表示： 其中 A 和 B 中的一个是由 R1 表示的 C1-30 的烃基，另一个是-(CH2)n-NR2R3；Y 是-CO-、-CONR5- 或-COO-；Z 是-O-、-OCO-、-OCONR6- 或-NR6-；R2 和 R3 分别代表氢、低级烷基、苯基或苄基，或共同代表具有 3-7 个成员的杂环；-(Y)1-A 和-Z-B 的-NR5-(CH2)n-NR2R3 和-NR6-(CH2)n-NR2R3 可以是以下 W 组： 其中环 E 是包括两个氮原子的 6 或 7 个成员的杂环，R2 是氢、低级烷基、苯基或苄基；R4 是氢、卤素、低级烷基、低级酰基、硝基、氰基、低级烷氧羰基、氨基甲酰基、低级烷基氨基甲酰基、低级烷氨基、低级酰氨基、低级烷氧基或低级酰氧基；R5和R6各自为氢、低级烷基、低级酰基、低级烷基氨基甲酰基或所述环E的一部分；l为0或1；m为2-5的整数；n为0-5的整数。1,2-二取代哌啶衍生物或其盐具有良好的促进毛发生长和再生的效果，可用于护理、改善或预防哺乳动物，尤其是人类的脱发。
• PREVENTIVES AND REMEDIES FOR HYPERPHOSPHATEMIA
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0972525A1

  公开（公告）日：2000-01-19

  This invention has for its object to provide a pharmaceutical composition for the prevention and/or treatment of hyperphosphatemia and secondary hyperparathyroidism, inclusive of their accessory disorders and symptoms. The object is accomplished by provision of a pharmaceutical composition comprising an adenosine antagonist as an active ingredient.

  本发明的目的是提供一种药物组合物，用于预防和/或治疗高磷血症和继发性甲状旁腺机能亢进症，包括其附属疾病和症状。 本发明的目的是提供一种药物组合物，其活性成分包括腺苷拮抗剂。