基于结构-活性关系 乙恶唑设计并合成了一系列的2-(2,6-二氟苯基)-4-(4-取代的苯基)-1,3-恶唑啉4a-y和苯甲酰基苯基脲。发现大多数这些化合物显示出优异的杀螨活性。当浓度为2.5 mg L -1时,它们对蜘蛛螨的卵和幼虫的死亡率都达到85%以上。一些化合物还表现出优异的杀虫活性。2,4-二苯基-1,3-恶唑啉的4-苯基上的取代基的位置和类型对活性有很大影响。2-(2,6-二氟苯基)-4-(2-Cl-4-(4-Cl-苯氧基)苯基)-1,3-恶唑啉(4r)在2.5 mg L -1下表现出100%的杀螨作用,对甜菜夜蛾和小菜蛾的死亡率分别为12.5 mg L -1和65%和93%,几乎与乙恶唑。新发现的结构-活性关系也可能有益于进一步的杀螨剂/杀虫剂开发。
[DE] SUBSTITUIERTE TETRAHYDROISOCHINOLINE ALS MMP-INHIBITOREN, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS MEDIKAMENT [EN] SUBSTITUTED TETRAHYDROISOCHINOLINES USED IN THE FORM OF MMP INHIBITORS, METHOD FOR THE PRODUCTION AND USE THEREOF IN THE FORM OF DRAGS [FR] TETRAHYDRO-ISOQUINOLEINES SUBSTITUEES, UTILISEES COMME INHIBITEURS MMP, LEUR PROCEDE DE FABRICATION ET LEUR UTILISATION COMME MEDICAMENTS
A Single Phosphine Ligand Allows Palladium-Catalyzed Intermolecular CO Bond Formation with Secondary and Primary Alcohols
作者:Xiaoxing Wu、Brett P. Fors、Stephen L. Buchwald
DOI:10.1002/anie.201104361
日期:2011.10.10
Forging a bond: An efficient, general palladium catalyst for CObond‐forming reactions of secondary and primaryalcohols with a range of aryl halides has been developed using the ligand 1. Heteroaryl halides, and for the first time, electron‐rich aryl halides can be coupled with secondaryalcohols. A diverse set of substrate combinations are possible with just a singleligand, thus obviating the need
形成键:使用配体1开发了一种高效、通用的钯催化剂,用于仲醇和伯醇与一系列芳基卤化物的C O 键形成反应。杂芳基卤化物和富电子芳基卤化物首次可以与仲醇偶联。只需一个配体即可实现多种底物组合,因此无需调查多个配体。
Copper-catalyzed oxidative trifluoroethoxylation of aryl boronic acids with CF 3 CH 2 OH
作者:Ke Zhang、Xiu-Hua Xu、Feng-Ling Qing
DOI:10.1016/j.jfluchem.2016.07.008
日期:2017.4
A mild and efficient copper-catalyzed oxidative trifluoroethoxylation of aryl and heteroaryl boronicacids with CF3CH2OH has been developed. This protocol tolerates a range of functional groups, allowing access to a variety of aryl and heteroaryl trifluoroethyl ethers.