1005206-25-6Relevant articles and documents
Catalytic borylation of SCF3-functionalized arenes by rhodium(I) boryl complexes: Regioselective C-H activation at the ortho-position
Kallaene, Sabrina I.,Braun, Thomas
, p. 9311 - 9315 (2014)
An unprecedented reaction pathway for the borylation of SCF 3-containing arenes using [Rh(Bpin)(PEt3)3] (pin=pinacolato) is reported. Catalytic processes were developed and the functionalizations proceed under mild reaction conditions. The C-H activations occur with a unique regioselectivity for the position ortho to the SCF 3 group, which apparently serves as directing group. Borylated SCF3 compounds can serve as versatile building blocks. SCF 3 building blocks: A unique reaction route allows access to SCF 3-functionalized arenes, which are borylated at the ortho-position. The functionalization proceeds by C-H borylation with [Rh(Bpin)(PEt 3)3] (pin=pinacolato), and the SCF3 group likely serves as directing group. The generated borylated SCF3 compounds are versatile building blocks for further transformations.
Discovery, Optimization, and Target Identification of Novel Potent Broad-Spectrum Antiviral Inhibitors
Yang, Yiqing,Cao, Lin,Gao, Hongying,Wu, Yue,Wang, Yaxin,Fang, Fang,Lan, Tianlong,Lou, Zhiyong,Rao, Yu
, p. 4056 - 4073 (2019/05/06)
Viral infections are increasing and probably long-lasting global risks. In this study, a chemical library was exploited by phenotypic screening to discover new antiviral inhibitors. After optimizations from hit to lead, a novel potent small molecule (RYL-634) was identified, showing excellent broad-spectrum inhibition activity against various pathogenic viruses, including hepatitis C virus, dengue virus, Zika virus, chikungunya virus, enterovirus 71, human immunodeficiency virus, respiratory syncytial virus, and others. The mechanism of action and potential targets of RYL-634 were further explored by the combination of activity-based protein profiling and other techniques. Finally, human dihydroorotate dehydrogenase was validated as the major target of RYL-634. We did not observe any mutant resistance under our pressure selections with RYL-634, and it had a strong synergistic effect with some Food and Drug Administration-approved drugs. Hence, there is great potential for developing new broad-spectrum antivirals based on RYL-634.
Efficient Rh-catalyzed C-H borylation of arene derivatives under photochemical conditions
Bheeter, Charles Beromeo,Chowdhury, Abhishek Dutta,Adam, Rosa,Jackstell, Ralf,Beller, Matthias
supporting information, p. 10336 - 10340 (2015/10/28)
Photocatalysis allows innovations in organic synthesis. Among the various catalytic reactions, CH-functionalizations offer valuable possibilities for the refinement of easily available building blocks. In this respect, catalytic borylation is of interest, too. So far, most of the catalytic borylation reactions are performed under thermal conditions at comparably high temperatures. Here, we describe a new synthetic route for efficient borylation reactions of arenes using a photocatalytic pathway. This novel approach allows the synthesis of a broad variety of borylated arenes and heteroarenes under mild conditions. Applying trans-[Rh(PMe3)2(CO)Cl] as an active photocatalyst and HBPin as an boron source, we achieved high TON. A catalytic cycle that relies on a Rh(i)-Rh(iii) interconversion is proposed.
