N-[2-[1-[2-[4-(p-toluidino)piperidin-1-yl]ethyl]cyclohexyl]ethyl]phthalimide | 518287-48-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: N-[2-[1-[2-[4-(p-toluidino)piperidin-1-yl]ethyl]cyclohexyl]ethyl]phthalimide
• 英文别名: 2-[2-[1-[2-[4-(4-methylanilino)piperidin-1-yl]ethyl]cyclohexyl]ethyl]isoindole-1,3-dione
• CAS: 518287-48-4
• 化学式: C₃₀H₃₉N₃O₂
• 分子量: 473.659
• InChiKey: ADHYGXXZBIFZEW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.8
• 重原子数：
  35
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  52.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  呋喃甲酰氯 、 N-[2-[1-[2-[4-(p-toluidino)piperidin-1-yl]ethyl]cyclohexyl]ethyl]phthalimide 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 以58%的产率得到N-[2-[1-[2-[4-[N-(p-tolyl)-2-furancarboxamide]piperidin-1-yl]ethyl]cyclohexyl]ethyl]phthalimide
  参考文献：
  名称：

  EP1621538

  摘要：

  公开号：
• 作为产物：
  描述：

  N-[2-[1-(Formylmethyl)cyclohexyl]ethyl]phthalimide 、 4-(p-toluidino)piperidine ditrifluoroacetate 在 三乙酰氧基硼氢化钠 、 溶剂黄146 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 1.5h， 生成 N-[2-[1-[2-[4-(p-toluidino)piperidin-1-yl]ethyl]cyclohexyl]ethyl]phthalimide
  参考文献：
  名称：

  NOVEL 4-(2FUROYL)AMINOPIPERIDINES, INTERMEDIATES IN SYNTHESIZING THE SAME, PROCESS FOR PRODUCING THE SAME AND MEDICINAL USE OF THE SAME

  摘要：

  公开号：

  EP1443046B1

文献信息

• 4-(2-Furoyl) aminopiperidine compound useful as therapeutic agent for itching
  申请人：Muraki Yukiko

  公开号：US20060270632A1

  公开（公告）日：2006-11-30

  There are provided compounds represented by the following general formula (I): [where R 1 is 5-methylpyridin-2-yl, p-tolyl or mesityl, R 2 is one of the following general formulas (II)-(IX): (where R 3 is C1-C4 alkyl, R 4 is H or C1-C4 alkyl, R 5 is H, 3-pyridylmethyl or 4-pyridylmethyl, and R 6 is 2,4-dihydroxybenzyl, 3-pyridylmethyl or 4-pyridylmethyl), or when R 1 is mesityl, R 2 is the following formula (X)], and pharmaceutically acceptable salts thereof. The compounds exhibit pruritus-inhibiting action, and are useful for prevention or treatment of itching and pruritus caused by reaction against insect-inflicted wounds, reaction against environmental allergens, skin infections or external parasite infections, or caused to renal dialysis patient.

  提供了以下通式（I）所代表的化合物：[其中R1为5-甲基吡啶-2-基、对甲基苯基或二甲基苯基，R2为以下通式（II）-（IX）之一：（其中R3为C1-C4烷基，R4为H或C1-C4烷基，R5为H、3-吡啶甲基或4-吡啶甲基，R6为2,4-二羟基苯甲基、3-吡啶甲基或4-吡啶甲基），或当R1为二甲基苯基时，R2为以下通式（X）]，以及其药学上可接受的盐。这些化合物具有抑制瘙痒作用，可用于预防或治疗由对昆虫造成的伤口反应、对环境过敏原的反应、皮肤感染或外部寄生虫感染引起的瘙痒和瘙痒，或透析患者引起的瘙痒。
• 4-(2-furoyl)aminopiperidine compound useful as therapeutic agent for itching
  申请人：Kyorin Pharmaceutical Co., Ltd

  公开号：US07601843B2

  公开（公告）日：2009-10-13

  There are provided compounds represented by the following general formula (I): [where R1 is 5-methylpyridin-2-yl, p-tolyl or mesityl, R2 is one of the following general formulas (II)-(IX): (where R3 is C1-C4 alkyl, R4 is H or C1-C4 alkyl, R5 is H, 3-pyridylmethyl or 4-pyridylmethyl, and R6 is 2,4-dihydroxybenzyl, 3-pyridylmethyl or 4-pyridylmethyl), or when R1 is mesityl, R2 is the following formula (X)], and pharmaceutically acceptable salts thereof. The compounds exhibit pruritus-inhibiting action, and are useful for prevention or of itching and pruritus caused by reaction against insect-inflicted wounds, reaction against environmental allergens, skin infections or external parasite infections, or caused to renal dialysis patient.

  以下是通用式（I）所代表的化合物：[其中R1是5-甲基吡啶-2-基，对甲基苯基或三甲基苯基，R2是以下通用式（II）-（IX）之一：（其中R3是C1-C4烷基，R4是H或C1-C4烷基，R5是H，3-吡啶甲基或4-吡啶甲基，R6是2,4-二羟基苯甲基，3-吡啶甲基或4-吡啶甲基），或当R1是三甲基苯基时，R2是以下式子（X）]，以及其药学上可接受的盐。这些化合物具有止痒作用，可用于预防或治疗由昆虫叮咬引起的瘙痒和瘙痒反应，环境过敏原引起的反应，皮肤感染或外部寄生虫感染引起的瘙痒，或透析患者引起的瘙痒。
• 4-(2-FUROYL)AMINOPIPERIDINE COMPOUND USEFUL AS THERAPEUTIC AGENT FOR ITCHING
  申请人：KYORIN PHARMACEUTICAL CO., LTD.

  公开号：EP1621538A1

  公开（公告）日：2006-02-01

  There are provided compounds represented by the following general formula (I): [where R1 is 5-methylpyridin-2-yl, p-tolyl or mesityl, R2 is one of the following general formulas (II)-(IX): (where R3 is C1-C4 alkyl, R4 is H or C1-C4 alkyl, R5 is H, 3-pyridylmethyl or 4-pyridylmethyl, and R6 is 2,4-dihydroxybenzyl, 3-pyridylmethyl or 4-pyridylmethyl), or when R1 is mesityl, R2 is the following formula (X)], and pharmaceutically acceptable salts thereof. The compounds exhibit pruritus-inhibiting action, and are useful for prevention or treatment of itching and pruritus caused by reaction against insect-inflicted wounds, reaction against environmental allergens, skin infections or external parasite infections, or caused to renal dialysis patient.

  本发明提供了由以下通式 (I) 代表的化合物： [其中 R1 为 5-甲基吡啶-2-基、对甲苯基或间甲基，R2 为以下通式 (II)-(IX) 之一： (其中 R3 是 C1-C4 烷基，R4 是 H 或 C1-C4 烷基，R5 是 H、3-吡啶甲基或 4-吡啶甲基，R6 是 2,4-二羟基苄基、3-吡啶甲基或 4-吡啶甲基）、 或当 R1 为甲苯甲基时，R2 为下式 (X)]、 及其药学上可接受的盐类。这些化合物具有抑制瘙痒的作用，可用于预防或治疗由昆虫造成的伤口反应、环境过敏原反应、皮肤感染或体外寄生虫感染引起的瘙痒，或肾透析患者引起的瘙痒。
• 4-(2-Furoyl) Aminopiperidine compound useful as therapeutic agent for itching
  申请人：Kyorin Pharmaceutical Co., Ltd.

  公开号：EP2325183A1

  公开（公告）日：2011-05-25

  There are provided compounds represented by the following general formula (I): where R1 is 5-methylpyridin-2-yl, p-tolyl or mesityl, R2 is where R3 is C1-C4 alkyl, R4 is H or C1-C4 alkyl, and pharmaceutically acceptable salts thereof. The compounds exhibit pruritus-inhibiting action, and are useful for prevention or treatment of itching and pruritus caused by reaction against insect-inflicted wounds, reaction against environmental allergens, skin infections or external parasite infections, or caused to renal dialysis patient.

  本发明提供了由以下通式 (I) 代表的化合物： 其中 R1 是 5-甲基吡啶-2-基、对甲苯基或间甲苯基，R2 是 其中 R3 是 C1-C4 烷基，R4 是 H 或 C1-C4 烷基、 及其药学上可接受的盐类。这些化合物具有抑制瘙痒的作用，可用于预防或治疗由昆虫造成的伤口反应、环境过敏原反应、皮肤感染或外部寄生虫感染引起的瘙痒，或肾透析患者引起的瘙痒。
• US7601843B2
  申请人：——

  公开号：US7601843B2

  公开（公告）日：2009-10-13