N-p-tolylpiperidin-3-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: N-p-tolylpiperidin-3-ol
• 英文别名: 1-(4-methylphenyl)piperidin-3-ol
• 化学式: C₁₂H₁₇NO
• 分子量: 191.273
• InChiKey: ZHPHKTWTILFZOC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  23.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  3-羟基哌啶 、 4-碘甲苯 在 copper(l) iodide caesium carbonate 作用下， 以 乙腈 为溶剂， 反应 18.0h， 以83%的产率得到N-p-tolylpiperidin-3-ol
  参考文献：
  名称：

  N- versus O-Arylation of Aminoalcohols:  Orthogonal Selectivity in Copper-Based Catalysts

  摘要：

  Two complementary protocols for copper-catalyzed arylation of aminoalcohols were developed. Selective N-arylation was accomplished at room temperature using 2-isobutyrylcyclohexanone (a beta-diketone) as supporting ligand, while selective O-arylation required the use of 3,4,7,8-tetramethylphenanthroline at 80-110 degrees C. Systematic examination of the reaction scope revealed that high levels of selectivity are achieved for a variety of substrates, provided that nonchelating (or weakly chelating) aminoalcohols are used. The generality of the method was highlighted by the synthesis, in a pairwise fashion, of a number of functionalized N- and O-arylated aminoalcohols.

  DOI：

  10.1021/ja068926f

文献信息

• 4-HETEROCYCLOALKYLPYRI(MI)DINES, PROCESS FOR THE PREPARATION THEREOF AND THEIR USE AS MEDICAMENTS
  申请人：Engelhardt Harald

  公开号：US20090203673A1

  公开（公告）日：2009-08-13

  The present invention encompasses compounds of general Formula (I) wherein X and R 1 to R 3 are defined as in claim 1 , which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.

  本发明涵盖一般式（I）中定义为权利要求1中定义的X和R1到R3的化合物，适用于治疗以细胞过度或异常增殖为特征的疾病，并且利用其制备具有上述特性的制药组合物。
• US8258129B2
  申请人：——

  公开号：US8258129B2

  公开（公告）日：2012-09-04
• [EN] COMPOSITIONS FOR THE TREATMENT OF DISEASE WITH IMMUNE STIMULATORY CONJUGATES<br/>[FR] COMPOSITIONS POUR LE TRAITEMENT D'UNE MALADIE AVEC DES CONJUGUÉS IMMUNOSTIMULANTS
  申请人：SILVERBACK THERAPEUTICS INC

  公开号：WO2020056008A1

  公开（公告）日：2020-03-19

  Methods and conjugates are disclosed for alleviating toxicity(ies) associated with administration of immune-stimulatory conjugates, and in particular for alleviating toxicity(ies) associated with intravenous administration of such conjugates.