6-pyrimidin-5-yl-hexan-1-ol | 88940-77-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 6-pyrimidin-5-yl-hexan-1-ol
• 英文别名: 5-pyrimidinehexanol；6-(Pyrimidin-5-YL)hexan-1-OL；6-pyrimidin-5-ylhexan-1-ol
• CAS: 88940-77-6
• 化学式: C₁₀H₁₆N₂O
• 分子量: 180.25
• InChiKey: QCXSNTXJIYUSLC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  13
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  46
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-pyrimidin-5-yl-hexan-1-ol 在 氯化亚砜 、 potassium iodide 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成 2-(6-嘧啶-5-基己基)异吲哚-1,3-二酮
  参考文献：
  名称：

  Pyrido[2,1-b]quinazolinecarboxamide derivatives as platelet activating factor antagonists

  摘要：

  A series of N-[(heteroaryl)alkyl]pyrido[2,1-b]quinazolines were evaluated for their ability to inhibit the binding of radiolabeled platelet activating factor (PAF) to its receptor on dog platelets. The most potent compounds in this series were found to be pyrido[2,1-b]quinazoline-8-carboxamides possessing a four- or six-carbon chain between the carboxamide nitrogen atom and a 3-pyridinyl or 5-pyrimidinyl moiety. Since earlier metabolism studies with pyridoquinazolinecarboxamides suggest that the carboxamide moiety is labile to hydrolysis in vivo, attempts were made to find isosteric replacements for this group. The substitutions examined led to a loss of activity; however, insertion of a methyl group on the carbon atom alpha to the carboxamide nitrogen led to an enantioselective enhancement of potency. (R)-2-(1-Methylethyl)-N-[1-methyl-4-(3-pyridinyl)butyl]-11-oxo-11H- pyrido[2,1-b]quinazoline-8-carboxamide (34) was more potent than the corresponding S enantiomer in the PAF binding assay and was also shown to be more resistant to degradation by amidases present in whole liver homogenates obtained from guinea pig, dog, and squirrel monkey. The corresponding rac-2-(1-methylethyl)-N-[1-methyl-4-(3-pyridinyl)butyl]-11-oxo-11H- pyrido[2,1-b]quinazoline-8-carboxamide (33) was found to inhibit transient PAF-induced thrombocytopenia and decreases in blood pressure in guinea pigs after intravenous or oral administration and to have a duration of action of greater than 5 h after an oral dose of 200 mg/kg. Compound 33 thus represents the prototype of a new class of orally active PAF antagonists.

  DOI：

  10.1021/jm00397a034
• 作为产物：
  描述：

  5-己炔-1-醇 生成 6-pyrimidin-5-yl-hexan-1-ol
  参考文献：
  名称：

  N-substituted diphenylpiperidines and antiobesity use thereof

  摘要：

  该化合物的公式为##STR1##其中R.sub.1是##STR2##星号表示与哌啶基团的特定配位取向；R.sub.2是烷基或--CO--(CH.sub.2).sub.n--其中n为0至11；R.sub.3和R.sub.4，独立地，是氢、卤素或低碳氧基；HET是吡啶基、嘧啶基或咪唑基，以及其与药用可接受酸的盐。公式I的化合物表现出降血糖活性，并可用作抗肥胖剂。

  公开号：

  US04632925A1

文献信息

• Pyrido[2,1-b]quinazoline derivatives useful as agents for treatment of
  申请人：Hoffmann-La Roche Inc.

  公开号：US04551460A1

  公开（公告）日：1985-11-05

  Pyrido[2,1-b]quinazoline derivatives of the formulas ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as hereinafter set forth, are described. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions as well as for the treatment of vascular disorders involving thrombosis.

  该文描述了化合物的结构公式为##STR1##其中R.sub.1、R.sub.2和R.sub.3如下所述的吡啶[2,1-b]喹唑啉衍生物。公式I和II的化合物可用作治疗过敏症状的药物，也可用于治疗涉及血栓形成的血管疾病。
• A general synthesis of alkylpyridines
  作者：Beatriz Iglesias、Rosana Alvarez、Angel R de Lera

  DOI：10.1016/s0040-4020(01)00170-3

  日期：2001.4

  The hydroboration of alkenes, followed by the coupling of the B-alkyl-9-borabicyclo[3.3.1]nonane derivatives with bromopyridines constitutes an efficient procedure for the attachment of functionalized alkyl chains to the pyridine nucleus.

  烯烃的硼氢化，然后将B-烷基-9-硼环[3.3.1]壬烷衍生物与溴吡啶偶联，是将官能化烷基链连接到吡啶核上的有效方法。
• Chloroaniline derivatives
  申请人：Glaxo Group Limited

  公开号：US05149698A1

  公开（公告）日：1992-09-22

  The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, wherein Q represents a chlorine atom or a trifluoromethyl group; X represents a bond, or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain, and Y represents a bond, or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain with the proviso that the sum total or carbon atoms in the chains X and Y is not more than 10, and the chains XCH.sub.2 and CH.sub.2 Y may each be optionally substituted by one or two C.sub.1-3 alkyl groups, or, when one carbon atom is substituted by two alkyl groups, these may be linked to form an alkylene group; R represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sup.1 and R.sup.2 each represent a hydrogen atom or a C.sub.1-3 alkyl group, with the proviso that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4; and Het is optionally substituted pyrimidinyl. The compounds have a stimulant action at .beta.-adrenoreceptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

  本发明提供了一般式(I)的化合物及其生理上可接受的盐和溶剂化物，其中Q代表氯原子或三氟甲基基团；X代表键或C.sub.1-6烷基，C.sub.2-6烯基或C.sub.2-6炔基链，Y代表键或C.sub.1-6烷基，C.sub.2-6烯基或C.sub.2-6炔基链，但X和Y链中的碳原子总数不超过10，且XCH.sub.2和CH.sub.2Y链各可选择性地被一个或两个C.sub.1-3烷基取代，或者当一个碳原子被两个烷基取代时，它们可以连接形成一个烷基链；R代表氢原子或C.sub.1-3烷基；R.sup.1和R.sup.2各代表氢原子或C.sub.1-3烷基，但R.sup.1和R.sup.2中的碳原子总数不超过4；Het是可选择性取代的嘧啶基。这些化合物在β-肾上腺素受体上具有刺激作用，可用于治疗与可逆性气道阻塞相关的疾病，如哮喘和慢性支气管炎。
• TILLEY, J. W.
  作者：TILLEY, J. W.

  DOI：——

  日期：——
• TILLEY, JEFFERSON W.;BURGHARD, BARBARA;BURGHARDT, CHARLES;MOWLES, THOMAS +, J. MED. CHEM., 31,(1988) N 2, 466-472
  作者：TILLEY, JEFFERSON W.、BURGHARD, BARBARA、BURGHARDT, CHARLES、MOWLES, THOMAS +

  DOI：——

  日期：——