17889-23-5Relevant academic research and scientific papers
Organoarsenic probes to study proteins by NMR spectroscopy
Adekoya, Ibidolapo,Huber, Thomas,Mahawaththa, Mithun C.,Nitsche, Christoph,Orton, Henry W.,Otting, Gottfried
supporting information, p. 701 - 704 (2022/01/25)
Arsenical probes enable structural studies of proteins. We report the first organoarsenic probes for nuclear magnetic resonance (NMR) and electron paramagnetic resonance (EPR) spectroscopy to study proteins in solutions. These probes can be attached to ir
Design, synthesis and identification of silicon-containing HCV NS5A inhibitors with pan-genotype activity
Liu, Baomin,Gai, Kuo,Qin, Hui,Liu, Xushi,Cao, Yuan,Lu, Qin,Lu, Dandan,Chen, Deyang,Shen, Hengqiao,Song, Wei,Zhang, Yang,Wang, Xiaojin,Xu, Hongjiang,Zhang, Yinsheng
, p. 95 - 105 (2018/02/20)
Modification of a HCV NS5A inhibitor, ombitasvir, led to the identification of 10d with improved pan-genotype NS5A inhibition and better pharmacokinetic properties. The key structural changes to ombitasvir include bioisosteric replacement of carbon with silicon atom. Compared with ombitasvir, the activity of anti-HCV genotypes (GT 1 to 6) of 10d is increased to some extent, especially the inhibitory activity against genotype 3a and 6a is increased by more than seven times, and the dog's in vivo pharmacokinetics properties were also superior to ombitasvir. Further drug evaluation showed that 10d was similar to ombitasvir on plasma protein binding and liver distribution profiles, with no cytotoxicity and no inhibitory effect on both CYP 450 and hERG ligand binding. However, permeability assay results indicated that 10d was not the substrate of P-gp or BCRP transporter, which is different from that of ombitasvir. The results of a 14-day repeat-dose toxicity study identified no toxicity with 10d. Our findings in preclinical tests suggest that the silicon-containing compound 10d could be worthy of continued study as a potential drug candidate.
AMIDE COMPOUND
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Paragraph 0466, (2016/08/17)
The present invention relates to compound (I) or a salt thereof which has a RORγt inhibitory action. In the formula (I), each symbol is as defined in the specification.
Heterocyclic compound
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Paragraph 0548, (2016/10/08)
The present invention relates to compound (I) or a salt thereof which has a ROR γ t inhibitory action. wherein each symbol is as defined in the specification.
Assembly of Primary (Hetero)Arylamines via CuI/Oxalic Diamide-Catalyzed Coupling of Aryl Chlorides and Ammonia
Fan, Mengyang,Zhou, Wei,Jiang, Yongwen,Ma, Dawei
supporting information, p. 5934 - 5937 (2015/12/11)
A general and practical catalytic system for aryl amination of aryl chlorides with aqueous or gaseous ammonia has been developed, with CuI as the catalyst and bisaryl oxalic diamides as the ligands. The reaction proceeds at 105-120°C to provide a diverse set of primary (hetero)aryl amines in high yields with various functional groups.
Mild and highly selective palladium-catalyzed monoarylation of ammonia enabled by the use of bulky biarylphosphine ligands and palladacycle precatalysts
Cheung, Chi Wai,Surry, David S.,Buchwald, Stephen L.
supporting information, p. 3734 - 3737 (2013/08/23)
A method for the Pd-catalyzed arylation of ammonia with a wide range of aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity for monoarylation of ammonia to primary arylamines was achieved under mild conditions or at rt by the use of bulky biarylphosphine ligands (L6, L7, and L4) as well as their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, and 3c). As this process requires neither the use of a glovebox nor high pressures of ammonia, it should be widely applicable.
Direct stereospecific amination of alkyl and aryl pinacol boronates
Mlynarski, Scott N.,Karns, Alexander S.,Morken, James P.
supporting information, p. 16449 - 16451,3 (2020/09/15)
The direct amination of alkyl and aryl pinacol boronates is accomplished with lithiated methoxyamine. This reaction directly provides aliphatic and aromatic amines, stereospecifically, and without preactivation of the boronate substrate.
Ipso-Fluorination of aryltrimethylsilanes using xenon difluoride
Lothian, Aileen P.,Ramsden, Christopher A.,Shaw, Maxine M.,Smith, Rachel G.
experimental part, p. 2788 - 2793 (2011/05/02)
Reaction of aryltrimethylsilanes with xenon difluoride in C 6F6/Pyrex at room temperature gives aryl fluorides in good yield. The reaction is inhibited when acetonitrile is used as solvent but proceeds well in CFCl3/Pyrex or CH 2Cl2/Pyrex. Pyrex appears to be a very effective heterogeneous catalyst for this ipso-fluorination. The reaction does not proceed in PTFE, quartz, soda glass or glassy-carbon flasks or Pyrex flasks pre-rinsed with 2 M NaOH. Aryltrimethylstannanes and arylboronic acids and their esters do not undergo ipso-fluorination under similar conditions. Plausible mechanisms involving electrophilic addition of polarised xenon difluoride [FXeδ+?F→Pyrex δ-] followed by ligand coupling are discussed.
PYRROLE-3-CARBOXAMIDE DERIVATIVES FOR THE TREATMENT OF OBESITY
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Page/Page column 12; 34, (2010/02/13)
The present invention relates to compounds of Formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Diphenylphosphinophenolate: A ligand for the palladium-catalysed silylation of aryl halides activating simultaneously both palladium and silicon
Shirakawa,Kurahashi,Yoshida,Hiyama
, p. 1895 - 1896 (2007/10/03)
Diphenylphosphinophenolate was found to be an effective ligand for the palladium-catalysed silylation of aryl halides, activating not only palladium but also silicon of a disilane, where aryl bromides and iodides having such substituents as methyl, methoxy, amino, ethoxycarbonyl, trifluoromethyl, formyl or phenyl are applicable to the reaction with hexamethyldisilane to give the corresponding trimethylsilylarenes.
