71225-69-9Relevant academic research and scientific papers
MODULATORS OF TREX1
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Paragraph 0090, (2021/01/29)
Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with TREX1.
Rhodium-catalyzed Synthesis of 1-Arylisoquinoline Derivatives through Annulative Coupling of 3-Aryl-1, 2-benzisoxazoles and Alkynes
Noguchi, Teppei,Nishii, Yuji,Miura, Masahiro
supporting information, p. 1512 - 1514 (2017/11/04)
Direct annulative coupling of 3-aryl-1, 2-benzisoxazoles and alkynes efficiently proceeds in the presence of a Cp?Rh(III) catalyst to produce 2-(1-isoquinolinyl)phenols of interest in medicinal chemistry as well as materials chemistry. The products may also be useful precursors of quinoline-based bidentate ligands.
Palladium-catalyzed ortho-selective C-H bond chlorination of aromatic ketones
Shan, Gang,Huang, Gui-Yi,Rao, Yu,Zhang, Hui
, p. 1236 - 1240 (2015/12/31)
A palladium-catalyzed ortho-selective C-H bond chlorination reaction for the preparation of 2-chloro aromatic ketones was described. Both electron-withdrawing and electron-donating groups on the aromatic rings are well tolerated under the optimized conditions. The 2-chloro aromatic ketones obtained by our method could be applied to synthesize the derivatives of 1H-indazole or benzo[d]isoxazole.
Synthesis, herbicidal evaluation, and structure-activity relationship of benzophenone oxime ether derivatives
Ma, Jimei,Ma, Mingwei,Sun, Linhao,Zeng, Zhen,Jiang, Hong
, (2015/10/05)
A novel series of benzophenone oxime ether derivatives with tertiary amine groups were synthesized and their herbicidal activities of 24 compounds against Oryza sativa, Sorghum sudanense, Brassica chinensis, and Amaranthus mangostanus L. were also evaluated. Most of these compounds exhibited significant inhibitory effect on root growth at 20 ppm. Based on the herbicidal activity data, computational Three-Dimensional Quantitative Structure-Activity Relationship (3D-QSAR) analysis and molecular docking were undertaken. CoMFA contour maps were generated for the design of benzophenone oxime ether analogues with enhancing activity.
Synthesis of 3-substituted indazoles and benzoisoxazoles via Pd-catalyzed cyclization reactions: application to the synthesis of nigellicine
Inamoto, Kiyofumi,Katsuno, Mika,Yoshino, Takashi,Arai, Yukari,Hiroya, Kou,Sakamoto, Takao
, p. 2695 - 2711 (2007/10/03)
Syntheses of 3-substituted indazoles and benzoisoxazoles were efficiently accomplished with the aid of Pd-catalyzed intramolecular carbon-nitrogen and carbon-oxygen bond formations. The catalyst system described herein allows the cyclization to proceed under very mild conditions and thus could be applied to a wide range of substrates with acid- or base-sensitive functional groups. A total synthesis for the indazole ring-containing natural product nigellicine is also described.
(Partial) agonist/antagonist properties of novel diarylalkyl carbamates on histamine H3 receptors
Sasse,Stark,Ligneau,Elz,Reidemeister,Ganellin,Schwartz,Schunack
, p. 1139 - 1149 (2007/10/03)
In the search for new ligands of the histamine H3 receptor, novel diarylalkyl carbamates (1-19 were synthesized as derivatives of 3-(1H- imidazol-4-yl)propanol and -ethanol. Carbamates were built up via isocyanates either from corresponding amines by reaction with diphosgene or from related carboxylic acid/diphenylphosphoryl azide and the alcoholic component. Sterically hindered amines were prepared in a two-step reaction sequence from corresponding ketones. Some of the title compounds showed (partial) agonist activity at the histamine H3 receptor in vitro and in vivo. Diphenylmethyl carbamate 2 was identified as a new lead structure (ED50 = 5.3 ± 2.6 mg/kg po, α = 1.0). Aromatic substitution in ortho- or para-positions of 2 led to a loss of agonist activity. meta-Substitution was tolerated to some extent. These effects seemed to be caused by steric rather than electronic properties of the substituents. An investigation of exchange of one or both phenyl rings of 2 by heterocyclic rings led to the highly active and selective thienyl derivative 18 (ED50 = 3.4 ± 1.4 mg/kg po, α = 1.0). These new (partial) agonists of the histamine H3 receptor might serve as pharmacological tools for investigating molecular aspects of the H3 receptor or as possible centrally acting therapeutic agents with oral bioavailability. (C) 2000 Elsevier Science Ltd.
Nitrile oxide-BF3 complex as electrophilic moiety towards aromatic systems: Stereospecific synthesis of oximes
Auricchio, Sergio,Bini, Antonella,Pastormerlo, Eros,Ricca, Aldo,Truscello, Ada M.
, p. 7589 - 7596 (2007/10/02)
Aromatic oximes are obtained stereospecifically by action of nitrile oxide-BF3 complexes on aromatic compounds.
