A palladium-catalyzedoxidative carbonylation of arylhydrazines and alkynes with balloon pressure CO/O2 to afford trisubstituted pyrazoles in a one-pot manner has been developed. The formation of trisubstituted pyrazoles involves a sequential C–N bond cleavage, carbonylation, Sonogashira coupling, Michael addition, and intramolecular condensation cyclization tandem process. An unprecedented oxidative
已经开发了用球罐压力CO / O 2进行钯催化的芳基肼和炔烃的氧化羰基化反应,以一锅法得到三取代的吡唑。三取代吡唑的形成涉及连续的C–N键断裂,羰基化,Sonogashira偶联,迈克尔加成和分子内缩合环化串联过程。芳基肼的空前的氧化Sonogashira-羰基化反应在如此简便的吡唑方法中起着关键作用。
Synthesis of Aryl Hydrazines via CuI/BMPO Catalyzed Cross-Coupling of Aryl Halides with Hydrazine Hydrate in Water
作者:Siripuram Vijay Kumar、Dawei Ma
DOI:10.1002/cjoc.201800326
日期:2018.11
The N,N’‐bis(2,6‐dimethylphenyl)oxalamide was discovered as a powerful ligand for Cu‐catalyzedcross‐coupling of arylhalides with hydrazine hydrate, leading to the formation of a variety of aryl hydrazines at 80 oC in water under the assistance of K3PO4 and 4 mol% cetyltrimethylammonium bromide from aryl bromides and aryl iodides. Good to excellent yields were observed in most cases.
的N,N-双(2,6-二甲基苯基)草酰胺,发现作为一个强大的配体对Cu催化的与水合肼芳基卤化物的交叉耦合,从而导致的各种芳基肼的形成在80 ö用C在K 3 PO 4和4 mol%的十六烷基三甲基溴化铵的帮助下,从芳基溴化物和芳基碘化物中加入水。在大多数情况下,观察到良好至极好的产量。
[EN] POLYAROMATIC UREA DERIVATIVES AND THEIR USE IN THE TREATMENT OF MUSCLE DISEASES<br/>[FR] DÉRIVÉS D'URÉE POLYAROMATIQUES ET LEUR UTILISATION DANS LE TRAITEMENT DE MALADIES MUSCULAIRES
申请人:ANAGENESIS BIOTECHNOLOGIES S A S
公开号:WO2021013712A1
公开(公告)日:2021-01-28
The current invention provides urea derivatives, in particular compounds having the core structure heteroaryl-NH-CO-NH-aryl-O- heteroaryl, for use in treating, ameliorating, delaying, curing and/ or preventing a disease or condition associated with muscle cells and/or satellite cells, such as Duchenne muscular dystrophy, Becker muscular dystrophy, cachexia or sarcopenia.
Regioselective α-arylation of coumarins and 2-pyridones with phenylhydrazines under transition-metal-free conditions
作者:Parul Chauhan、Makthala Ravi、Shikha Singh、Prashant Prajapati、Prem P. Yadav
DOI:10.1039/c5ra20954d
日期:——
A transition-metal-free regioselective α-arylation of coumarins and 2-pyridones has been accomplished by the reaction of phenylhydrazines with coumarins or 2-pyridones.
一种无过渡金属的选择性α-芳基化反应已经成功实现,通过苯基肼与香豆素或2-吡啶酮的反应。
Regulated activation of cell-membrane receptors by metal-chelating agonists
申请人:——
公开号:US20040053299A1
公开(公告)日:2004-03-18
Invented is a regulated activation of cell-membrane receptors by small molecule agents. Also invented is a method to render a cell-membrane receptor responsive to the activation by small molecule compounds by specific single point mutations in the transmembrane region.