1-Acetyl-1,2,3,6-tetrahydro-4-tributylstannyl-pyridine | 130579-43-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 1-Acetyl-1,2,3,6-tetrahydro-4-tributylstannyl-pyridine
• 英文别名: 1-acetyl-1,2,5,6-tetrahydro-4-(tri-n-butylstannyl)pyridine；1,2,3,6-tetrahydro-1-acetyl-4-tributylstannylpyridine；1-acetyl-4-tributylstannyl-1,2,3,6-tetrahydropyridine；1-[4-(Tributylstannyl)-3,6-dihydropyridin-1(2H)-yl]ethan-1-one；1-(4-tributylstannyl-3,6-dihydro-2H-pyridin-1-yl)ethanone
• CAS: 130579-43-0
• 化学式: C₁₉H₃₇NOSn
• 分子量: 414.219
• InChiKey: WQNMPPIJMRVCEN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.55
• 重原子数：
  22
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.84
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  1-Acetyl-1,2,3,6-tetrahydro-4-tributylstannyl-pyridine 在 bis-triphenylphosphine-palladium(II) chloride 盐酸 、 2,6-二叔丁基-4-甲基苯酚 作用下， 以 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 反应 170.0h， 生成 7-(1-Acetyl-1,2,3,6-tetrahydro-pyridin-4-yl)-1-(2,4-difluoro-phenyl)-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid
  参考文献：
  名称：

  新型的7-取代的喹诺酮类抗菌剂。7-烯基，环烯基和1,2,3,6-四氢-4-吡啶基-1,8-萘啶的合成†

  摘要：

  已经实现了在C-7位置带有碳-碳键，无环或环状乙烯基取代基的1,8-萘啶类抗菌剂的会聚合成。合成方法基于7-氯-1,8-萘啶与适当取代的有机锡试剂的钯催化交叉偶联。

  DOI：

  10.1002/jhet.5570280133
• 作为产物：
  描述：

  1-acetyl-4-hydroxy-4-(tributylstannyl)piperidine 、 甲基磺酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 1-Acetyl-1,2,3,6-tetrahydro-4-tributylstannyl-pyridine
  参考文献：
  名称：

  Preparation of certain 7-substituted quinolones

  摘要：

  披露了将烷基、烯基、炔基或芳基基团耦合到喹啉和萘啶的七个位置的新工艺。还描述了具有抗菌活性的新型中间体和最终化合物，以及用于相同用途的制剂。

  公开号：

  US04945160A1

文献信息

• Synthesis of 7-(alkenyl, cycloalkenyl, and 1,2,3,6-tetrahydro-4-pyridinyl)quinolones
  作者：John S. Kiely、Edgardo Laborde、Lawrence E. Lesheski、Ruth A. Bucsh

  DOI：10.1002/jhet.5570280621

  日期：1991.10

  in which the C-7 position is substituted with a vinyl, a 1-cyclopentenyl, or a 1,2,3,6-tetrahydro-4-pyridinyl group. These quinolones were synthesized via a palladium-catalyzed cross coupling of a 7-quinolyltriflate with an appropriately functionalized vinylstannane.

  制备了一系列的1-环丙基-1,4-二氢-4-氧代喹啉，其中C-7位置被乙烯基，1-环戊烯基或1,2,3,6-四氢-4-取代吡啶基。这些喹诺酮是通过钯催化的7-喹啉滤液与适当官能化的乙烯基锡烷的交叉偶联而合成的。
• Isothiazoloquinolones and related compounds as anti-infective agents
  申请人：Bradbury James Barton

  公开号：US20050075363A1

  公开（公告）日：2005-04-07

  The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , R 2 , R 3 , R 5 , R 6 , R 7 , A 8 and R 9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

  本发明提供了式I和式II的化合物和盐：它们具有抗微生物活性。本发明还提供了有用于制备式I和式II化合物的新型合成中间体。其中变量A1、R2、R3、R5、R6、R7、A8和R9在此有定义。本文所披露的式I和式II的某些化合物是细菌DNA合成和细菌复制的有效和选择性抑制剂。本发明还提供了抗微生物组合物，包括含有一个或多个式I或式II化合物和一个或多个载体、赋形剂或稀释剂的制药组合物。这样的组合物可能仅包含式I或式II的化合物作为唯一活性剂，也可能包含式I或式II的化合物和一个或多个其他活性剂的组合。本发明还提供了治疗动物微生物感染的方法。
• Piperidine compounds
  申请人：ADIR ET COMPAGNIE

  公开号：US20020161228A1

  公开（公告）日：2002-10-31

  A compound selected from those of formula (I): 1 wherein: W represents optionally substituted naphthyl, or group of formula Y 2 as defined in the description, n represents an integer from 1 to 6 inclusive, Z represents single bond, oxygen, or optionally substituted nitrogen, A and Q each represent CH or nitrogen, M, together with carbon of phenyl to which it is bonded, represents thienyl, furyl, pyrrolyl or oxopyrrolyl, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same are useful in the treatment of some CNS disorders.

  从式(I)中选择的化合物：其中：W代表可选取代的萘基或式Y2所定义的基团，n表示从1到6的整数，包括Z代表单键，氧或可选取代的氮，A和Q各自代表CH或氮，M与其结合的苯环上的碳一起，代表噻吩基，呋喃基，吡咯基或氧代吡咯基，其异构体和药学上可接受的酸或碱加盐物，以及含有它们的药物制品在治疗某些中枢神经系统疾病方面是有用的。
• Pyridine compounds
  申请人：Les Laboratoires Servier

  公开号：US06399616B1

  公开（公告）日：2002-06-04

  A compound selected from those of formula (I): wherein: W represents optionally substituted naphthyl, n represents an integer from 2 to 3 inclusive, Z represents a single bond, A represents nitrogen, Q represents nitrogen, M, together with the carbon of pyridyl to which it is bonded, represents thieno, furo, pyrrolo or oxopyrrolo, Its optical isomers and pharmaceutically-acceptable acid or base additional salts thereof, and Medicinal products containing the same which are useful in the treatment of CNS disorders. It being understood that “aryl” is phenyl, naphthyl, dihydronaphthyl, or tetrahydronaphthyl.

  从式(I)中选择的化合物：其中：W表示可选取代的萘基，n表示从2到3的整数，Z表示单键，A表示氮，Q表示氮，M与其结合的吡啶基的碳一起表示噻吩基，呋喃基，吡咯基或氧代吡咯基，其光学异构体和药学上可接受的酸或碱附加盐，以及包含它们的治疗中枢神经系统疾病的药物制剂。其中，“芳基”是苯基，萘基，二氢萘基或四氢萘基。
• New isothiazoloquinolones and related compounds as anti-infective agents
  申请人：Bradbury James Barton

  公开号：US20060235041A1

  公开（公告）日：2006-10-19

  The invention provides certain compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , R 2 , R 3 , R 5 , R 6 , R 7 , A 8 and R 9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

  本发明提供了公式I和公式II的某些化合物和盐：具有抗微生物活性。本发明还提供了在制备公式I和公式II的化合物中有用的新型合成中间体。本文中定义了变量A1、R2、R3、R5、R6、R7、A8和R9。本文披露的公式I和公式II的某些化合物是细菌DNA合成和细菌复制的有效和选择性抑制剂。本发明还提供了抗微生物组合物，包括制药组合物，其中包含一个或多个公式I或公式II的化合物和一个或多个载体、赋形剂或稀释剂。这样的组合物可以仅包含公式I或公式II的化合物作为唯一的活性剂，也可以包含公式I或公式II的化合物和一个或多个其他活性剂的组合物。本发明还提供了治疗动物微生物感染的方法。