26388-13-6Relevant academic research and scientific papers
Monodisperse CuPd alloy nanoparticles as efficient and reusable catalyst for the C (sp2)–H bond activation
Huang, Fei,Wang, Feifan,Hu, Qiyan,Tang, Lin,Xu, Dongping,Fang, Yang,Zhang, Wu
, (2021/03/17)
Metal-catalyzed selective activation of C–H bonds is very important for the construction of a variety of biologically active molecules. Supported alloy nanoparticles are of great interest in various catalytic applications due to the synergistic effects between different metals. Here, well-dispersed CuPd alloy nanoparticles supported on reduced graphene oxide (rGO) were synthesized and found to be highly efficient and recyclable catalyst for the chelation-assisted C (sp2)–H bond activation. Aromatic ketones or esters were synthesized via the cross-dehydrogenative coupling (CDC) reaction between 2-arylpyridines and alcohols or acids. Moreover, the catalyst was recovered and used for five times without significantly losing activity.
CYANO-SUBTITUTED HETEROCYCLES WITH ACTIVITY AS INHIBITORS OF USP30
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Page/Page column 48; 49, (2018/04/17)
The present invention relates to a class of cyano-substituted-heterocycles of Formula (I) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility in a variety of therapeutic areas including cancer and conditions involving mitochondrial dysfunction. (I)
Exploring Tandem Ruthenium-Catalyzed Hydrogen Transfer and SNAr Chemistry
Polidano, Kurt,Reed-Berendt, Benjamin G.,Basset, Ana?s,Watson, Andrew J. A.,Williams, Jonathan M. J.,Morrill, Louis C.
, p. 6716 - 6719 (2017/12/26)
A hydrogen-transfer strategy for the catalytic functionalization of benzylic alcohols via electronic arene activation, accessing a diverse range of bespoke diaryl ethers and aryl amines in excellent isolated yields (38 examples, 70% average yield), is reported. Taking advantage of the hydrogen-transfer approach, the oxidation level of the functionalized products can be selected by judicious choice of simple and inexpensive additives.
Transition-metal-free intramolecular carbene aromatic substitution/Büchner reaction: Synthesis of fluorenes and [6,5,7]benzo-fused rings
Liu, Zhenxing,Tan, Haocheng,Wang, Long,Fu, Tianren,Xia, Ying,Zhang, Yan,Wang, Jianbo
supporting information, p. 3056 - 3060 (2015/03/30)
Intramolecular aromatic substitution and Büchner reaction have been established as powerful methods for the construction of polycyclic compounds. These reactions are traditionally catalyzed by RhII catalysts with a-diazocarbonyl compounds as the substrates. Herein a transition-metal-free intramolecular aromatic substitution/Büchner reaction is presented. These reactions use readily available N-tosylhydrazones as the diazo compound precursors and show wide substrate scope.
Graphene oxide grafted with Pd17Se15 nano-particles generated from a single source precursor as a recyclable and efficient catalyst for C-O coupling in O-arylation at room temperature
Joshi, Hemant,Sharma, Kamal Nayan,Sharma, Alpesh K.,Prakash, Om,Singh, Ajai Kumar
supporting information, p. 7483 - 7485 (2013/08/23)
The Pd17Se15 nanoparticles, synthesized for the first time from a single source precursor [Pd(L)Cl2] {L = 1,3-bis(phenylselenyl)propan-2-ol} and grafted onto graphene oxide, show high catalytic activity in C-O coupling between aryl/heteroaryl chlorides/bromides and phenol at room temperature (Pd loading 1 mol%; yield up to 94%).
(2-Pyridyl)acetone-promoted Cu-catalyzed O-arylation of phenols with aryl iodides, bromides, and chlorides
Zhang, Qi,Wang, Deping,Wang, Xianyang,Ding, Ke
supporting information; experimental part, p. 7187 - 7190 (2009/12/09)
(Chemical Equation Presented) Employing (2-pyridyl)acetone as a new supporting ligand, the copper-catalyzed coupling reactions of aryl chlorides, aryl bromides, and aryl iodides with various phenols successfully proceeded in good yields under mild conditions. This reaction displays great functional groups compatibility and excellent reactive selectivity.
A study of the gas-phase interconversion of 1-(2-aryloxyphenyl)-alkaniminyl and 2-(aryliminomethyl)phenoxyl radicals
Black, Michael,Cadogan,Leardini, Rino,McNab, Hamish,McDougald, Graham,Nanni, Daniele,Reed, David,Zompatori, Alberto
, p. 1825 - 1832 (2007/10/03)
Flash vacuum pyrolysis of the allyl ethers 9-11 and of the oxime ethers 15-17 at 650°C (5 × 10-2-5 × 10-3 Torr) generates 2-(aryliminomethyl)phenoxyl radicals 4 and 1-(2-aryloxyphenyl)alkaniminyl radicals 5 respectively which can interconvert via a spirodienyl radical leading to common products which are generally isolated in low to moderate yield. The iminyls 5 normally undergo β-cleavage leading to nitriles (e.g. 21) and/or to benzofurans (e.g. 22) after cyclisation. The phenoxyls 4 show more complex behaviour dominated by hydrogen abstraction processes leading to products such as phenols (e.g. 32), the indole 27 or phenanthridines 34 and 35.
(Aryloxy)aryl semicarbazones and related compounds: A novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen
Dimmock, Jonathan R.,Puthucode, Ramanan N.,Smith, Jennifer M.,Hetherington, Mark,Quail, J. Wilson,Pugazhenthi, Uma,Lechler, Terry,Stables, James P.
, p. 3984 - 3997 (2007/10/03)
A number of (aryloxy)aryl semicarbazones and related compounds were synthesized and evaluated far anticonvulsant activities. After intraperitoneal injection to mice, the semicarbazones were examined in the maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ), and neurotoxicity (NT) screens. The results indicated that greater protection was obtained in the MES test than the scPTZ screen. Quantitation of approximately one-third of the compounds revealed an average protection index (PI, i.e. TD50/ED50) of approximately 9. After oral administration to rats, a number of compounds displayed significant potencies in the MES screen (ED50 of 1-5 mg/kg) accompanied by very high protection indices. In fact over half the compounds had PI figures of greater than 100, and two were in excess of 300. The compounds were essentially inactive in the scPTZ and NT screens after oral administration to rats. Various compounds displayed greater potencies and PI figures in the mouse intraperitoneal and rat oral screens than three reference clinically used drugs. The data generated supported a binding site hypothesis. Quantitative structure-activity relationships indicated a number of physicochemical parameters which contributed to activity in the MES screen. X-ray crystallography of five compounds suggested the importance of certain interatomic distances and bond angles for activity in the mouse and rat MES screens.
Affinity of 10-(4-Methylpiperazino)dibenzoxepins for Clozapine and Spiroperidol Binding Sites in Rat Brain
Harris, Terry W.,Smith, Howard E.,Mobley, Philip L.,Manier, D. Hal,Sulser, Fridolin
, p. 855 - 858 (2007/10/02)
10-(4-Methylpiperazino)dibenzoxepins were prepared and evaluated as potential antipsychotic agents using specific clozapine diazepine> binding sites in rat forebrain that are noncholinergic and nondopaminergic in nature and from which clozapine is displaced by known antipsychotic agents. Clozapine binding in the presence of atropine represents nonmuscarinic binding, while binding in the absence of atropine represents muscarinic (cholinergic) plus nonmuscarinic binding.The relative affinity for dopamine binding sites was determined by displacement of spiroperidol from binding sites in rat caudate nuclei.Thus, clozapine, its 2-chloro isomer, its dechloro analogue, and their 5H-dibenzocycloheptene and dibenzoxepin analogues have about the same relative affinity for the nonmuscarinic clozapine binding sites.At the spiroperidol (dopaminergic) sites, both the nature of the tricyclic system and the presence of chlorine atom on the tricyclic system have a substantial effect on the binding affinity.Within each series, shift of a chlorine atom from the position distal to the piperazino group to the proximal position increases the binding affinity by a factor of about nine, but removal of the chlorine atom substantially decreases the binding affinity.Nevertheless, 10-(4-methylpiperazino)dibenzoxepin has a threefold greater affinity for the dopaminergic binding sites than does clozapine itself.
