- Enantioselective Synthesis of Biaryl Atropisomers by Pd-Catalyzed C?H Olefination using Chiral Spiro Phosphoric Acid Ligands
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The discovery of proper ligands to simultaneously modulate the reactivity and effectively control the stereoselectivity is a central topic in the field of enantioselective C?H activation. Herein, we reported the synthesis of axially chiral biaryls by Pd-catalyzed atroposelective C?H olefination. A novel chiral spiro phosphoric acid, STRIP, was identified as a superior ligand for this transformation. A broad range of axially chiral quinoline derivatives were synthesized in good yields with excellent enantioselectivities (up to 98 % ee). Density functional theory was used to gain a theoretical understanding of the enantioselectivities in this reaction.
- Luo, Jun,Zhang, Tao,Wang, Lei,Liao, Gang,Yao, Qi-Jun,Wu, Yong-Jie,Zhan, Bei-Bei,Lan, Yu,Lin, Xu-Feng,Shi, Bing-Feng
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supporting information
p. 6708 - 6712
(2019/04/26)
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- METHODS AND COMPOSITIONS FOR TREATING INFECTION
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Provided herein are compositions and methods for treating or preventing infection.
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Paragraph 0289
(2015/09/28)
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- Br?nsted acid-mediated intramolecular cyclization of biaryl triazenes for the synthesis of fluorenes and 9,10-dihydro-phenanthrenes
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The efficient synthesis of fluorenes from biaryl triazenes is successfully developed. Up to 27 examples of biaryl triazenes are converted into their corresponding fluorene derivatives in the presence of CF3COOH (4.0 equiv). Mechanism research i
- Xu, Lijun,Yang, Weijun,Zhang, Lili,Miao, Maozhong,Yang, Zhigen,Xu, Xin,Ren, Hongjun
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p. 9206 - 9221
(2015/01/08)
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- Repurposing the antihistamine terfenadine for antimicrobial activity against staphylococcus aureus
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Staphylococcus aureus is a rapidly growing health threat in the U.S., with resistance to several commonly prescribed treatments. A high-throughput screen identified the antihistamine terfenadine to possess, previously unreported, antimicrobial activity against S. aureus and other Gram-positive bacteria. In an effort to repurpose this drug, structure-activity relationship studies yielded 84 terfenadine-based analogues with several modifications providing increased activity versus S. aureus and other bacterial pathogens, including Mycobacterium tuberculosis. Mechanism of action studies revealed these compounds to exert their antibacterial effects, at least in part, through inhibition of the bacterial type II topoisomerases. This scaffold suffers from hERG liabilities which were not remedied through this round of optimization; however, given the overall improvement in activity of the set, terfenadine-based analogues provide a novel structural class of antimicrobial compounds with potential for further characterization as part of the continuing process to meet the current need for new antibiotics.
- Perlmutter, Jessamyn I.,Forbes, Lauren T.,Krysan, Damian J.,Ebsworth-Mojica, Katherine,Colquhoun, Jennifer M.,Wang, Jenna L.,Dunman, Paul M.,Flaherty, Daniel P.
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supporting information
p. 8540 - 8562
(2014/12/11)
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- Intermolecular mizoroki-heck reaction of aliphatic olefins with high selectivity for substitution at the internal position
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New ligand for old reaction: The title reaction of aryltriflates with aliphatic olefins leads to substitution at the internal position with high selectivity. The ratio of the desired isomer (shown in the scheme) to the sum of all other isomers is generall
- Qin, Liena,Ren, Xinfeng,Lu, Yunpeng,Li, Yongxin,Zhou, Jianrong
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supporting information; experimental part
p. 5915 - 5919
(2012/07/30)
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