We describe a method for intramolecular desulfonylative coupling using bis(cyclooctadiene)nickel as a catalyst. A broad range of aromatic, heteroaromatic and aliphatic sulfones can be utilized as substrates in this process. This method provides an atom‐economical route to the synthesis of various biaryls and an efficient tool for the catalytic conversion of sulfonyl groups, representing a significant
Acetamide as Cocatalyst for the Nitrogen-Directed Coupling of Arenes with Aryl Chlorides through Ruthenium-Catalyzed C-H Activation
作者:Jie Zhang、Qin Yang、Zhu Zhu、Mao Lin Yuan、Hai Yan Fu、Xue Li Zheng、Hua Chen、Rui Xiang Li
DOI:10.1002/ejoc.201201127
日期:2012.12
by C–H activation is described. Acetamide was found to be an effective cocatalyst for this generally applicable ruthenium(II)-catalyzed direct arylation reaction. A wide range of deactivated aryl chlorides could be efficiently coupled under the mild temperature of 101 °C. The new process is highly atom-economical and sustainable.
描述了一种通过 C-H 活化交叉偶联芳烃的简单高效的方法。发现乙酰胺是这种普遍适用的钌 (II) 催化的直接芳基化反应的有效助催化剂。在 101 °C 的温和温度下,可以有效地偶联多种失活的芳基氯。新工艺具有高度的原子经济性和可持续性。
Combination of RuCl<sub>3</sub>·xH<sub>2</sub>O with PEG – a simple and recyclable catalytic system for direct arylation of heteroarenes via C–H bond activation
作者:Lei Jian、Hai-Yu He、Jin Huang、Qian-Hui Wu、Mao-Lin Yuan、Hai-Yan Fu、Xue-Li Zheng、Hua Chen、Rui-Xiang Li
DOI:10.1039/c7ra02638b
日期:——
A simple and recyclable catalytic system for directarylation of heteroarenes via C–H bond activation was developed with a relatively inexpensive RuCl3·xH2O as a catalyst and PEG-400 as a green medium without any additive or ligand. This system not only showed excellent functional group compatibility, but also the ratio of mono- to diarylated product was easily regulated by varying the reaction conditions
通过使用相对便宜的RuCl 3 · x H 2 O作为催化剂和PEG-400作为绿色介质,没有任何添加剂或配体,开发了一种简单且可回收的催化系统,用于通过C–H键活化杂芳烃直接芳基化。该体系不仅显示出优异的官能团相容性,而且通过改变反应条件也很容易调节单芳基化产物与二芳基化产物的比例。而且,该转化可以在空气中进行,并且在0.3mol%的低催化剂负载下可以容易地按比例放大至克级。特别地,在将该催化剂循环六次之后,获得了85%的良好产率。
[EN] 4-OXO-1H-QUINOLINE-3-CARBOXAMIDES AS MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS<br/>[FR] 4-OXO-1H-QUINOLINE-3-CARBOXAMIDES UTILES COMME MODULATEURS DES TRANSPORTEURS DE CASSETTE SE LIANT À L'ATP
申请人:VERTEX PHARMA
公开号:WO2011072241A9
公开(公告)日:2012-06-14
[EN] The present invention relates to 4-oxo-1H-quinoline-3-carboxamides as modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. [FR] La présente invention concerne des 4-oxo-1H-quinoline-3-carboxamides utiles comme modulateurs des transporteurs de cassette se liant à l'ATP ( » ABC ») ou de leurs fragments, notamment le régulateur de la conductance transmembranaire de la mucoviscidose. L'invention concerne également des compositions contenant les composés de l'invention et des méthodes associées. En outre, la présente invention concerne des méthodes de traitement de maladies induites par les transporteurs ABC au moyen de ces modulateurs.