42881-66-3Relevant articles and documents
Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety
Li, Linsen,Okumu, Antony,Dellos-Nolan, Sheri,Li, Zoe,Karmahapatra, Soumendrakrishna,English, Anthony,Yalowich, Jack C.,Wozniak, Daniel J.,Mitton-Fry, Mark J.
, p. 2477 - 2480 (2018)
Novel bacterial type II topoisomerase inhibitors (NBTIs) constitute a promising new class of antibacterial agents. We report a series of NBTIs with potent anti-staphylococcal activity and diminished hERG inhibition. Dioxane-linked compound 9 demonstrated MICs ≤1 μg/mL against both methicillin-susceptible (MSSA) and -resistant Staphylococcus aureus (MRSA), accompanied by reduced hERG inhibition as compared to cyclohexane- or piperidine-linked analogs.
Direct access of the chiral quinolinyl core of cinchona alkaloids via a br?nsted acid and chiral amine co-catalyzed chemo- and enantioselective α-alkylation of quinolinylmethanols with enals
Tong, Mengchao,Wang, Sinan,Zhuang, Jinchen,Qin, Cong,Li, Hao,Wang, Wei
supporting information, p. 1195 - 1199 (2018/02/23)
A strategy for the facile construction of the chiral quinolinylmethanolic structure, a core featured in cinchona alkaloids, is reported. A new reactivity is harnessed by TfOH-promoted chemoselective activation of α-C-H over O-H bond in quinolinylmethanols. The new reactivity is successfully engineered with an iminium catalysis in a synergistic manner to create a powerful conjugate addition-cyclization cascade process for synthesis of chiral quinoline derived π-butyrolactones in good yields and with good to excellent enantioselectivities. The method enables the first total synthesis of natural product broussonetine in three steps.
Flexible palladium-catalysed amidation reactions for the synthesis of complex aryl amides
Barfoot, Christopher,Brooks, Gerald,Brown, Pamela,Dabbs, Steven,Davies, David T.,Giordano, Ilaria,Hennessy, Alan,Jones, Graham,Markwell, Roger,Miles, Timothy,Pearson, Neil,Smethurst, Christian A.
body text, p. 2685 - 2689 (2010/06/21)
This Letter describes the synthesis of complex aryl amides using palladium-catalysed amidation reactions. Use of these conditions allowed for the coupling of a variety of aryl halides and triflates with a host of primary amides in high yields.
