7062-64-8Relevant articles and documents
Targeting Chikungunya Virus Replication by Benzoannulene Inhibitors
Ahmed, S. Kaleem,Haese, Nicole N.,Cowan, Jaden T.,Pathak, Vibha,Moukha-Chafiq, Omar,Smith, Valerie J.,Rodzinak, Kevin J.,Ahmad, Fahim,Zhang, Sixue,Bonin, Kiley M.,Streblow, Aaron D.,Streblow, Cassilyn E.,Kreklywich, Craig N.,Morrison, Clayton,Sarkar, Sanjay,Moorman, Nathaniel,Sander, Wes,Allen, Robbie,Defilippis, Victor,Tekwani, Babu L.,Wu, Mousheng,Hirsch, Alec J.,Smith, Jessica L.,Tower, Nichole A.,Rasmussen, Lynn,Bostwick, Robert,Maddry, Joseph A.,Ananthan, Subramaniam,Gerdes, John M,Augelli-Szafran, Corinne E.,Suto, Mark J.,Morrison, Thomas E.,Heise, Mark T.,Streblow, Daniel N.,Pathak, Ashish K.
, p. 4762 - 4786 (2021)
A benzo[6]annulene, 4-(tert-butyl)-N-(3-methoxy-5,6,7,8-tetrahydronaphthalen-2-yl) benzamide (1a), was identified as an inhibitor against Chikungunya virus (CHIKV) with antiviral activity EC90 = 1.45 μM and viral titer reduction (VTR) of 2.5 log at 10 μM
Nature of the Nucleophilic Oxygenation Reagent Is Key to Acid-Free Gold-Catalyzed Conversion of Terminal and Internal Alkynes to 1,2-Dicarbonyls
Dubovtsev, Alexey Yu.,Shcherbakov, Nikolay V.,Dar'in, Dmitry V.,Kukushkin, Vadim Yu.
, p. 745 - 757 (2020/02/04)
2,3-Dichloropyridine N-oxide, a novel oxygen transfer reagent, allows the conductance of the gold(I)-catalyzed oxidation of alkynes to 1,2-dicarbonyls in the absence of any acid additives and under mild conditions to furnish the target species, including those derivatized by highly acid-sensitive groups. The developed strategy is effective for a wide range of alkyne substrates such as terminal- and internal alkynes, ynamides, alkynyl ethers/thioethers, and even unsubstituted acetylene (40 examples; yields up to 99%). The oxidation was successfully integrated into the trapping of reactive dicarbonyls by one-pot heterocyclization and into the synthesis of six-membered azaheterocycles. This synthetic acid-free route was also successfully applied for the total synthesis of a natural 1,2-diketone.
Iridium-Catalyzed Asymmetric Hydrogenation of Unsaturated Piperazin-2-ones
Wang, Yanzhao,Liu, Yuanyuan,Li, Kun,Yang, Guoqiang,Zhang, Wanbin
supporting information, p. 1933 - 1941 (2017/06/09)
Two different iridium catalyst systems, generated from the ruthenocene-based phosphine-oxazoline ligand tBu-mono-RuPHOX or the diphosphine ligand BINAP, were developed for the asymmetric hydrogenation of 5,6-dihydropyrazin-2(1H)-ones, affording chiral piperazin-2-ones in good yields and with moderate to good ees. Different catalytic behaviors for the hydrogenation of these types of substrate were observed with these two catalyst systems. Our tBu-mono-RuPHOX ligand, which bears a ruthenocene scaffold with planar chirality, was found to be the best ligand for the [Ir(L)(COD)]BArF catalyst system, affording the desired products with up to 94% ee. (Figure presented.).