4-tert-Butyl-4-piperidinol | 73617-82-0

• 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: 4-tert-Butyl-4-piperidinol
• 英文别名: 4-Tert-butylpiperidin-4-ol
• CAS: 73617-82-0
• 化学式: C₉H₁₉NO
• 分子量: 157.256
• InChiKey: BMPBHKNEDRNHJI-UHFFFAOYSA-N

物化性质

• 沸点：
  228.6±15.0 °C(Predicted)
• 密度：
  0.957±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  11
• 可旋转键数：
  1
• 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：

  10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-carboxylic acid chloride 、 4-tert-Butyl-4-piperidinol 生成 4-tert-butyl-1-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)carbonyl]-4-piperidinol
  参考文献：
  名称：

  KUKLA M. J.; BLOSS J. L.; BROUGHAM L. R., J. MED. CHEM., 1979, 22, NO 4, 401-406

  摘要：

  DOI：
• 作为产物：
  描述：

  1-Benzyl-4-tert-butyl-4-piperidinol 在 palladium on activated charcoal 氢气 作用下， 以 甲醇 为溶剂， 反应 50.0h， 以79%的产率得到4-tert-Butyl-4-piperidinol
  参考文献：
  名称：

  作为抗骨质疏松剂的（哌啶子基亚甲基）双（膦酸）衍生物的合成与评价。

  摘要：

  制备了一些（哌啶子基亚甲基）双（膦酸）衍生物，并评估了它们抑制甲状旁腺切除的大鼠的甲状旁腺激素诱导的血清钙升高的活性。几种（4-亚烷基-，4,4-二烷基-或4-烷基-4-卤代哌啶亚基）双（膦酸）衍生物表现出相当大的抑制活性。但是在哌啶环上具有芳族和极性取代基如叠氮基，羟基，氨基和酰胺基的化合物通常是无活性的。在这项研究中，两种4-亚烷基化合物（8a和8b）和4,4-环二烷基化合物（61）在静脉内或经口给药时均显示出强大的活性。

  DOI：

  10.1248/cpb.41.1971

文献信息

• NOVEL HETEROCYCLYL COMPOUNDS
  申请人：Aebi Johannes

  公开号：US20110092698A1

  公开（公告）日：2011-04-21

  The invention is concerned with novel bicyclic compounds of formula (I), wherein n, m, p, A, L, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 7 , R 8 , R 9 , and R 10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor may be used, for example, in the prevention and/or treatment of inflammatory diseases, particularly peripheral arterial occlusive diseases or atherothrombosis.

  这项发明涉及式(I)的新颖双环化合物，其中n、m、p、A、L、R1、R2、R3、R4、R5、R6、R7、R7、R8、R9和R10如描述和索赔中所定义，并且其生理上可接受的盐。这些化合物是CCR2受体、CCR5受体和/或CCR3受体的拮抗剂，例如可用于预防和/或治疗炎症性疾病，特别是外周动脉闭塞疾病或动脉粥样硬化形成。
• 1-[(10,11-Dihydro-5H-dibenzo[a,d]-cyclohepten-5-yl)methyl]-4-substituted
  申请人：G. D. Searle & Co.

  公开号：US04188485A1

  公开（公告）日：1980-02-12

  The invention encompasses 1-[10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)methyl]-4-substituted piperidines and related compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable acid addition salts thereof; wherein R in each occurrence represents hydrogen, halogen, alkyl radical of 1 to 7 carbon atoms, or trifluoromethyl, alike or different; R.sup.1 is hydrogen or alkyl radical of 1 to 7 carbon atoms; Z is hydroxy or NR.sup.2 R.sup.3 group wherein R.sup.2 and R.sup.3 are each hydrogen or alkyl radical of 1 to 7 carbon atoms or R.sup.2 and R.sup.3 together with the N-atom represent an azamonocyclic ring which contains from 4 to 6 carbon atoms; X is ethylene, vinylene, oxy or thio; and m and n are each alike or different integer from 1 to 4 inclusive; and 1-(2,2-diarylethyl)-4-piperidinols of the formula ##STR2## and the non-toxic pharmaceutically acceptable acid addition salts thereof; wherein Ar is phenyl optionally substituted with one or more halogen or alkyl radical of 1 to 7 carbon atoms, alike or different; Ar.sup.1 is phenyl optionally substituted with one or more halogen or alkyl radical of 1 to 7 carbon atoms alike or different; and R.sup.4 is selected from the group consisting of hydrogen alkyl radical of 1 to 7 carbon atoms, 4-hydroxy-1-(2,2-diphenylethyl)-3-piperidinyl, and 4-oxo-1-(2,2-diphenylethyl)-3-piperidinyl. These compounds possess utility as neuroleptic agents.

  本发明涉及公式为##STR1##的1-[10,11-二氢-5H-二苯并[a,d]环庚烯-5-基)甲基]-4-取代哌啶和相关化合物的非毒性药学上可接受的酸加成盐；其中R在每次出现时表示氢、卤素、1至7个碳原子的烷基基团或三氟甲基，相同或不同；R.sup.1是氢或1至7个碳原子的烷基基团；Z是羟基或NR.sup.2 R.sup.3基团，其中R.sup.2和R.sup.3分别是氢或1至7个碳原子的烷基基团，或者R.sup.2和R.sup.3与N原子一起表示含有4至6个碳原子的氮杂单环环；X是乙烯基、乙烯基、氧或硫；m和n是各自相同或不同的1至4个整数；以及公式为##STR2##的1-(2,2-二芳基乙基)-4-哌啶醇及其非毒性药学上可接受的酸加成盐；其中Ar是苯基，可选地取代一个或多个卤素或1至7个碳原子的烷基基团，相同或不同；Ar.sup.1是苯基，可选地取代一个或多个卤素或1至7个碳原子的烷基基团，相同或不同；R.sup.4选自羟基、1-(2,2-二苯基乙基)-4-哌啶基和4-氧代-1-(2,2-二苯基乙基)-3-哌啶基的群。这些化合物具有神经精神药物的功效。
• Intermediate products for producing oxazolidinone-quinolone hybrids
  申请人：Hubschwerlen Christian

  公开号：US20090306389A1

  公开（公告）日：2009-12-10

  The present invention describes intermediates (ZP) for a novel and efficient synthesis of compounds in which the pharmacophores of quinolone and oxazolidinone are linked to one another by way of a chemically stable linker.

  本发明描述了一种中间体（ZP），用于一种新颖有效的化合物合成，其中喹诺酮和噁唑烷酮的药效团通过化学稳定的连接剂相互连接。
• INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF
  申请人：Mizuno Kazuhiro

  公开号：US20140057895A1

  公开（公告）日：2014-02-27

  The present invention relates to a novel indazole- or pyrrolopyridine-derivative comprising a 5 membered heterocyclic substituent at 1 position thereof which has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same.

  本发明涉及一种新型吲唑或吡咯吡啶衍生物，其在1位具有一个5成员杂环取代基，具有对5-羟色胺-4受体的激动作用或部分激动作用，以及包含该衍生物的药物组合物。
• Condensed-ring pyrimidylamino derivative, preparation method therefor, and intermediate, pharmaceutical composition and applications thereof
  申请人：GUANGZHOU MAXINOVEL PHARMACEUTICALS CO., LTD.

  公开号：US10259816B2

  公开（公告）日：2019-04-16

  Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b′ to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.

  本发明公开了一种缩合环嘧啶基氨基衍生物、其制备方法、中间体、药物组合物及其应用。缩环嘧啶基氨基衍生物的制备方法包括：在溶剂中，在含钯催化剂存在下，使式I-a代表的化合物和式I-b′代表的化合物发生偶联反应，然后通过脱保护反应制备式I代表的化合物。还公开了缩合环嘧啶基氨基衍生物在制备预防、缓解和/或治疗由无性淋巴瘤激酶引起的肿瘤或疾病的药物中的应用。本发明的缩合环嘧啶基氨基衍生物对无性淋巴瘤激酶有明显的抑制作用。