tributyl(2,6-difluorophenyl)stannane

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: tributyl(2,6-difluorophenyl)stannane
• 英文别名: (2,6-difluorophenyl)tributyltin；2,6-Difluorophenyltributyltin；tributyl-(2,6-difluorophenyl)stannane
• 化学式: C₁₈H₃₀F₂Sn
• 分子量: 403.143
• InChiKey: DLTHSKKNYFFRAQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.02
• 重原子数：
  21
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  tributyl(2,6-difluorophenyl)stannane 在 四(三苯基膦)钯 、 一水合肼 作用下， 以 甲醇 、 xylene 为溶剂， 反应 24.0h， 生成 5-(2,6-difluorophenyl)nicotinoyl hydrazide
  参考文献：
  名称：

  Biarylcarbamoylindolines Are Novel and Selective 5-HT_2C Receptor Inverse Agonists:  Identification of 5-Methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a Potential Antidepressant/Anxiolytic Agent

  摘要：

  The evolution, synthesis, and biological activity of a novel series of 5-HT2C receptor inverse agonists are reported. Biarylcarbamoylindolines have been identified with excellent 5-HT2C affinity and selectivity over 5-HT2A receptors. In addition, (pyridyloxypyridyl)carbamoylindolines have been discovered with additional selectivity over the closely related 5-HT2B receptor. Compounds from this series are inverse agonists at the human cloned 5-HT2C receptor, completely abolishing basal activity in a functional assay. The new series have reduced P450 inhibitory liability compared to a previously described series of 1-(3-pyridylcarbamoyl)indolines (Bromidge et al. J. Med. Chem. 1998, 41, 1598) from which they evolved. Compounds from this series showed excellent oral activity in a rat mCPP hypolocomotion model and in animal models of anxiety. On the basis of their favorable biological profile, 32 (SB-228357) and 40 (SB-243213) have been selected for further evaluation to determine their therapeutic potential for the treatment of CNS disorders such as depression and anxiety.

  DOI：

  10.1021/jm990388c
• 作为产物：
  描述：

  1,3-二氟苯 、 三丁基氯化锡 在 正丁基锂 作用下， 以 四氢呋喃 、 正己烷 为溶剂， 反应 4.0h， 以88.6%的产率得到tributyl(2,6-difluorophenyl)stannane
  参考文献：
  名称：

  用于制备 2,6-双（二苯基膦）溴苯和相关双（氧化膦）的有机锡路线。新型配体的前体

  摘要：

  2,6-二氟苯基三烷基锡烷2,6-F 2 C 6 H 3 SnR 3 ( 1，R=Me；2，R=Bu)由商业产品制备。使用Ph 2 PLi，1和2进行亲核取代得到2,6-双(二苯基膦基)苯基三烷基锡烷2,6-(Ph 2 P) 2 C 6 H 3 SnR 3 ( 3 , R=Me; 4 , R=卜）。的反应3与Ñ正丁基锂和BRCH 2 CH 2Br得到2,6-双(二苯基膦基)溴苯(2,6-(Ph 2 P) 2 C 6 H 3 Br, 5 )，其氧化得到相关的双(氧化膦) 2,6-[Ph 2 P(O)] 2 C 6 H 3 Br ( 6 )。5与n- BuLi反应生成 2,6-双(二苯基膦基)苯基锂、2,6-(Ph 2 P) 2 C 6 H 3 Li ( 7 )。尝试制备相关的双（氧化膦）2,6-[Ph 2 P(O)] 2来自6 的C 6 H 3 Li ( 8 )在低温下以类似的方式受到分解的

  DOI：

  10.1002/zaac.202100210

文献信息

• Pyranodipyridine Compound
  申请人：Eisai R&D Management Co., Ltd.

  公开号：US20170137436A1

  公开（公告）日：2017-05-18

  Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof:

  由化学式(I)到(XXII)表示的化合物或其药用可接受的盐：
• Copper-catalyzed arylstannylation of arynes in a sequence
  作者：Hideya Tanaka、Hitoshi Kuriki、Teruhiko Kubo、Itaru Osaka、Hiroto Yoshida

  DOI：10.1039/c9cc02738f

  日期：——

  Copper-catalyzed arylstannylation of arynes has been developed. This transformation enables variously substituted ortho-stannylbiaryls and teraryls to be constructed straightforwardly. An electron-deficient tin center is the key, and thus the single or dual insertion of arynes into arylstannanes is precisely controllable by simply changing the equivalence of aryne precursors.

  已经开发了铜催化的芳烃的芳基甲锡烷基化。该转化使得可以直接构建各种取代的邻-锡烷基二芳基和三芳基。缺电子的锡中心是关键，因此，只需简单地改变芳烃前体的当量，即可精确控制芳烃单芳基或双芳烃的插入。
• Catalytic C−H Bond Stannylation: A New Regioselective Pathway to C−Sn Bonds via C−H Bond Functionalization
  作者：Meghan E. Doster、Jillian A. Hatnean、Tamara Jeftic、Sunjay Modi、Samuel A. Johnson

  DOI：10.1021/ja105588v

  日期：2010.9.1

  ubiquitous Stille coupling reaction utilizes Sn-C bonds and is of great utility to organic chemists. Unlike the B-C bonds used in the Miyaura-Suzuki coupling reaction, which are readily obtained via direct borylation of C-H bonds, routes to organotin compounds via direct C-H bond functionalization are lacking. Here we report that the nickel-catalyzed reaction of fluorinated arenes and pyridines with vinyl

  无处不在的 Stille 偶联反应利用 Sn-C 键，对有机化学家非常有用。与 Miyaura-Suzuki 偶联反应中使用的 BC 键不同，BC 键很容易通过 CH 键的直接硼酸化获得，但缺乏通过直接 CH 键官能化获得有机锡化合物的途径。在这里，我们报告氟化芳烃和吡啶与乙烯基锡烷的镍催化反应没有通过 CF 活化提供预期的乙烯基化合物，而是通过 CH 官能化提供新的 Sn-C 键，同时失去乙烯。这种机制为将 CH 键直接转化为碳-杂原子键提供了一种新的出乎意料的方法。
• Tetracyclic compound
  申请人：Kyowa Hakko Kogyo Co., Ltd.

  公开号：US05646283A1

  公开（公告）日：1997-07-08

  This invention relates to a novel tetracyclic compound represented by formula (I): ##STR1## or its pharmacologically-acceptable salt. The compound of this invention has strong immunosuppressive activity, and is useful as an immunosuppressive agent and as an agent for treating autoimmune disease.

  本发明涉及一种新型四环化合物，其化学式为(I): ##STR1## 或其药学上可接受的盐。该化合物具有强烈的免疫抑制活性，可作为免疫抑制剂和治疗自身免疫性疾病的药物。
• Indole derivatives as 5-HT receptor antagonist
  申请人：SmithKline Beecham p.l.c.

  公开号：US20030105139A1

  公开（公告）日：2003-06-05

  The invention relates to heterocyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders such as anxiety.

  本发明涉及具有药理活性的杂环化合物，其制备过程，含有它们的组合物以及它们在治疗中枢神经系统疾病如焦虑症方面的应用。