1073353-89-5Relevant academic research and scientific papers
Intramolecular aryl-aryl coupling: Via C-F bond activation tolerant towards C-I functionality
Steiner, Ann-Kristin,Feofanov, Mikhail,Amsharov, Konstantin
, p. 14377 - 14380 (2020)
Herein we report a transition-metal free activation of a particularly stable aromatic carbon-fluorine bond allowing intramolecular aryl-aryl coupling which is orthogonal to carbon-iodine functionality.
COMPOUNDS FOR TREATMENT OF EYE DISORDERS
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Page/Page column 78, (2021/01/23)
Compounds of formula I as defined herein, or pharmaceutically acceptable salts, solvates or derivatives thereof, are potent inhibitors of angiogenesis and accordingly are of use in the treatment and prevention of various angiogenesis-related disorders such as cancer.
HETEROCYCLIC COMPOUNDS AS PI3K-y INHIBITORS
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Paragraph 1347; 1348, (2018/02/28)
This application relates to compounds of Formula (I): or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
Synthesis of trimethylstannyl arylboronate compounds by sandmeyer-type transformations and their applications in chemoselective cross-coupling reactions
Qiu, Di,Wang, Shuai,Tang, Shengbo,Meng, He,Jin, Liang,Mo, Fanyang,Zhang, Yan,Wang, Jianbo
, p. 1979 - 1988 (2014/04/03)
A synthetic method based on Sandmeyer-type reactions to access both tin- and boron-substituted arenes from nitroaniline derivatives is described. This transformation can be applied to the synthesis of a series of functionalized trimethylstannyl arylboronates. In addition, the chemoselective reaction of the Stille and Suzuki-Miyaura cross-coupling reactions is explored, and a series of m- and p-terphenyl derivatives have been synthesized by conducting consecutive one-pot Stille and Suzuki-Miyaura cross-coupling reactions.
Expanding the palette of phenanthridinium cations
Cairns, Andrew G.,Senn, Hans Martin,Murphy, Michael P.,Hartley, Richard C.
supporting information, p. 3742 - 3751 (2014/04/03)
5,6-Disubstituted phenanthridinium cations have a range of redox, fluorescence and biological properties. Some properties rely on phenanthridiniums intercalating into DNA, but the use of these cations as exomarkers for the reactive oxygen species (ROS), superoxide, and as inhibitors of acetylcholine esterase (AChE) do not require intercalation. A versatile modular synthesis of 5,6-disubstituted phenanthridiniums that introduces diversity by Suzuki-Miyaura coupling, imine formation and microwave-assisted cyclisation is presented. Computational modelling at the density functional theory (DFT) level reveals that the novel displacement of the aryl halide by an acyclic N-alkylimine proceeds by an SNAr mechanism rather than electrocyclisation. It is found that the displacement of halide is concerted and there is no stable Meisenheimer intermediate, provided the calculations consistently use a polarisable solvent model and a diffuse basis set.
Antileishmanial bis-arylimidamides: DB766 analogs modified in the linker region and bis-arylimidamide structure-activity relationships
Reid, Carolyn S.,Zhu, Xiaohua,Pandharkar, Trupti,Werbovetz, Karl A.,Farahat, Abdelbasset A.,Boykin, David W.
supporting information, p. 6806 - 6810,5 (2020/09/02)
Analogs of the lead antileishmanial bis-arylimidamide DB766 were prepared that possess unsymmetrical substitutions on the diphenylfuran linker, and an additional compound was synthesized that contains isopropoxy groups meta to the central furan. These agents all displayed nanomolar in vitro potency against intracellular Leishmania with selectivity indexes >100 compared to J774 macrophages. While the unsymmetrical analogs were toxic to mice when given ip at 30 mg/kg/day, the compound bearing the meta isopropoxy groups was well tolerated by mice and showed activity in a murine model of visceral leishmaniasis when administered ip at 30 mg/kg/day for five days.
