1-(4-hydroxyphenyl)piperidin-4-ol

• 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: 1-(4-hydroxyphenyl)piperidin-4-ol
• 英文别名: 1-(4-hydroxyphenyl)-4-hydroxypiperidine
• 化学式: C₁₁H₁₅NO₂
• 分子量: 193.246
• InChiKey: UCWWJVDABCVIEN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  43.7
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  4-羟基哌啶 、 1,4-环己二酮 在 silica gel 、 正己烷 、 乙酸乙酯 作用下， 以 乙醇 为溶剂， 反应 9.0h， 以0.218 g of 1-(4-hydroxyphenyl)-4-hydroxypiperidine was obtained (yield 56.48%)的产率得到1-(4-hydroxyphenyl)piperidin-4-ol
  参考文献：
  名称：

  Method of producing aminophenol compounds

  摘要：

  本发明提供了一种工业上优越的方法，通过简单易行的程序高产高纯度地制备由式（1）表示的氨基苯酚化合物。本发明提供了一种制备由式（1）表示的氨基苯酚化合物的方法：（其中R1和R2中的每一个，可以相同或不同，是氢原子，取代或未取代的低碳基团等；R1和R2与相邻氮原子结合，可以形成具有或不具有其他介于杂原子的5-或6-成员杂环；该杂环可以被1至3个取代基取代，所述取代基选自羟基、取代或未取代的低碳基团、取代或未取代的芳基团、取代或未取代的芳氧基团等；并且式（1）中的羟基取代在苯环上的氨基基团的2-或4-位置），其中包括在中性或碱性条件下使由式（2）表示的环己酮二酮化合物与由式（3）表示的胺化合物（其中R1和R2如上所定义）反应。

  公开号：

  US07750156B2

文献信息

• [EN] METHOD OF PRODUCING AMINOPHENOL COMPOUNDS<br/>[FR] PROCEDE DE FABRICATION DE COMPOSES AMINOPHENOLS
  申请人：OTSUKA PHARMA CO LTD

  公开号：WO2005092832A1

  公开（公告）日：2005-10-06

  The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R1 and R2, taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R1 and R2 are as defined above), under a neutral or basic condition.

  本发明提供一种在高产率和高纯度下通过简单易行的程序生产由式（1）表示的氨基酚化合物的工业上有利的方法。本发明提供了一种生产由式（1）表示的氨基酚化合物的方法：（其中R1和R2中的每一个，可能相同也可能不同，是氢原子，取代或未取代的较低烷基基团或类似物；R1和R2与相邻氮原子一起可以形成5或6成员的杂环，有或无其他插入的杂原子；该杂环可以被1至3个取代基取代，所述取代基选自羟基团、取代或未取代的较低烷基基团、取代或未取代的芳基基团、取代或未取代的芳氧基团等；并且在式（1）中的羟基团被取代在苯环上的氨基团的2-或4-位置），其包括使由式（2）表示的环己二酮化合物与由式（3）表示的胺化合物（其中R1和R2如上定义）在中性或碱性条件下反应。
• Method of Producing Aminophenol Compounds
  申请人：Kiyokawa Hiroshi

  公开号：US20070219374A1

  公开（公告）日：2007-09-20

  The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R 1 and R 2 , which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R 1 and R 2 , taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R 1 and R 2 are as defined above), under a neutral or basic condition.

  本发明提供了一种工业上有利的方法，通过简单易行的步骤以高产率和高纯度生产由公式（1）表示的氨基酚化合物。本发明提供了一种制备由公式（1）表示的氨基酚化合物的方法：（其中R1和R2中的每一个，可以相同也可以不同，是氢原子，取代或未取代的低级烷基或类似物；R1和R2与相邻的氮原子一起，可以形成带有或不带其他杂原子的5-或6-成员杂环；该杂环可以被1至3个取代基所取代，所述取代基选自羟基，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳氧基等；公式（1）中的羟基被取代在苯环上的氨基的2-或4-位置），其中包括在中性或碱性条件下使由公式（2）表示的环己酮二酮化合物与由公式（3）表示的胺化合物（其中R1和R2如上所定义）反应。
• Method of producing aminophenol compounds
  申请人：Otsuka Pharmaceutical Co., Ltd.

  公开号：US07750156B2

  公开（公告）日：2010-07-06

  The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R1 and R2, taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R1 and R2 are as defined above), under a neutral or basic condition.

  本发明提供了一种工业上优越的方法，通过简单易行的程序高产高纯度地制备由式（1）表示的氨基苯酚化合物。本发明提供了一种制备由式（1）表示的氨基苯酚化合物的方法：（其中R1和R2中的每一个，可以相同或不同，是氢原子，取代或未取代的低碳基团等；R1和R2与相邻氮原子结合，可以形成具有或不具有其他介于杂原子的5-或6-成员杂环；该杂环可以被1至3个取代基取代，所述取代基选自羟基、取代或未取代的低碳基团、取代或未取代的芳基团、取代或未取代的芳氧基团等；并且式（1）中的羟基取代在苯环上的氨基基团的2-或4-位置），其中包括在中性或碱性条件下使由式（2）表示的环己酮二酮化合物与由式（3）表示的胺化合物（其中R1和R2如上所定义）反应。
• METHOD OF PRODUCING AMINOPHENOL COMPOUNDS
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：EP1727782A1

  公开（公告）日：2006-12-06
• US7750156B2
  申请人：——

  公开号：US7750156B2

  公开（公告）日：2010-07-06