166329-43-7Relevant academic research and scientific papers
Photoredox-Catalyzed Trifluoromethylative Intramolecular Cyclization: Synthesis of CF3-Containing Heterocyclic Compounds
Han, Hong Sik,Oh, Eun Hye,Jung, Young-Sik,Han, Soo Bong
, p. 1698 - 1702 (2018/04/16)
A general photoredox-catalyzed intramolecular cyclization was developed for the synthesis of trifluoromethylated heterocyclic compounds. The reaction proceeded smoothly under mild photocatalytic conditions with high functional group tolerance, allowing the preparation of oxygen-, sulfur-, or nitrogen-containing heterocycles of different sizes. The broad substrate scope demonstrated the complexity-building potential of the strategy.
Tandem Gold-Catalyzed Dehydrative Cyclization/Diels-Alder Reactions: Facile Access to Indolocarbazole Alkaloids
Borrero, Nicholas V.,Deratt, Lindsey G.,Ferreira Barbosa, Lais,Abboud, Khalil A.,Aponick, Aaron
, p. 1754 - 1757 (2015/04/14)
A gold-catalyzed synthesis of cyclic 2-oxodienes from readily prepared propargyl alcohols and the subsequent Diels-Alder reaction are reported. The dehydrative cyclization reactions proceeded smoothly, and the dienes formed in situ were demonstrated to un
The application of a monolithic triphenylphosphine reagent for conducting Appel reactions in flow microreactors
Roper, Kimberley A.,Lange, Heiko,Polyzos, Anastasios,Berry, Malcolm B.,Baxendale, Ian R.,Ley, Steven V.
supporting information; experimental part, p. 1648 - 1655 (2012/02/04)
Herein we describe the application of a monolithic triphenylphosphine reagent to the Appel reaction in flow-chemistry processi to generate various brominated products with high purity and in excellent yields, and with no requirement for further off-line pu fication.
Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use
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Page/Page column 57, (2009/09/07)
This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R′, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.
Construction of Azacycles Based on Endo-Mode Cyclization of Allenes
Mukai, Chisato,Kobayashi, Minoru,Kubota, Shoko,Takahashi, Yukie,Kitagaki, Shinji
, p. 2128 - 2136 (2007/10/03)
A new procedure for constructing monocyclic five- and six-membered azacycles by the endo-mode ring-closing reaction of allenylazido derivatives under neutral conditions has been developed. The azabicyclo[m.n.0] compounds were prepared by applying this newly developed procedure. The seven-membered azacycle was prepared when the allene possessing an unsubstituted carboxyl amido functionality was submitted to the basic conditions. In addition, indole and quinoline skeletons were synthesized using this procedure.
Antimicrobial effects of novel siderophores linked to β-lactam antibiotics
Kline,Fromhold,McKennon,Cai,Treiberg,Ihle,Sherman,Schwan,Hickey,Warrener,Witte,Brody,Goltry,Barker,Anderson,Tanaka,Shawar,Nguyen,Langhorne,Bigelow,Embuscado,Naeemi
, p. 73 - 93 (2007/10/03)
As a strategy to increase the penetration of antibiotic drugs through the outer membrane of Gram-negative pathogens, facilitated transport through siderophore receptors has been frequently exploited. Hydroxamic acids, catechols, or very close isosteres of catechols, which are mimics of naturally occurring siderophores, have been used successfully as covalently linked escorting moieties, but a much wider diversity of iron binding motifs exists. This observation, coupled to the relative lack of specificity of siderophore receptors, prompted us to initiate a program to identify novel, noncatechol siderophoric structures. We screened over 300 compounds for their ability to (1) support growth in low iron medium of a Pseudomonas aeruginosa siderophore biosynthesis deletion mutant, or (2) compete with a bactericidal siderophore-antibiotic conjugate for siderophore receptor access. From these assays we identified a set of small molecules that fulfilled one or both of these criteria. We then synthesized these compounds with functional groups suitable for attachment to both monobactam and cephalosporin core structures. Siderophore-β-lactam conjugates then were tested against a panel of Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus strains. Although several of the resultant chimeric compounds had antimicrobial activity approaching that of ceftazidime, and most compounds demonstrated very potent activity against their cellular targets, only a single compound was obtained that had enhanced, siderophore-mediated antibacterial activity. Results with tonB mutants frequently showed increased rather than decreased susceptibilities, suggesting that multiple factors influenced the intracellular concentration of the drugs. (C) 2000 Elsevier Science Ltd.
Synthesis of 1,4-benzodiazepine-1-carbothioamides, bicyclic analogues of the TIBO-type anti-HIV agents
Liu,Dodd
, p. 523 - 528 (2007/10/02)
A series of N'-substituted 1,4-benzodiazepine-1-carbothioamides 2a-j were prepared by reacting the precursor 1,4-benzodiazepine 11 with the corresponding N-substituted isothiocyanates 2a-i or with sodium thiocyanate-trifluoroacetic acid (2j). Despite the
