57631-05-7Relevant academic research and scientific papers
A straightforward access to 3-trifluoromethyl-1H-indazoles via (3+2)-cycloaddition of arynes with nitrile imines derived from trifluoroacetonitrile
Kowalczyk, Anna,Utecht-Jarzyńska, Greta,Mlostoń, Grzegorz,Jasiński, Marcin
, (2020/12/15)
In situ generated arynes react with nitrile imines derived from trifluoroacetonitrile at 0 °C in THF solutions yielding 3-trifluoromethyl-1H-indazole derivatives as the only intermolecular products. The reaction corresponds the expected (3 + 2)-cycloaddit
COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEROF IN MEDICINE
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, (2009/01/24)
Compound of formula (I) and salts thereof are provided: wherein X, Y, Z, R1, R2 and R3 are as defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt
Zhu, Gui-Dong,Gong, Jianchun,Gandhi, Viraj B.,Woods, Keith,Luo, Yan,Liu, Xuesong,Guan, Ran,Klinghofer, Vered,Johnson, Eric F.,Stoll, Vincent S.,Mamo, Mulugeta,Li, Qun,Rosenberg, Saul H.,Giranda, Vincent L.
, p. 2441 - 2452 (2007/10/03)
Thr-211 is one of three different amino acid residues in the kinase domain of protein kinase B/Akt as compared to protein kinase A (PKA), a closely related analog in the same AGC family. In an attempt to improve the potency and selectivity of our indazole-pyridine series of Akt inhibitors over PKA, efforts have focused on the incorporation of a chemical functionality to interact with the hydroxy group of Thr-211. Several substituents including an oxygen anion, amino, and nitro groups have been introduced at the C-6 position of the indazole scaffold, leading to a significant drop in Akt potency. Incorporation of a nitrogen atom into the phenyl ring at the same position (i.e., 9f) maintained the Akt activity and, in some cases, improved the selectivity over PKA. The structure-activity relationships of the new pyridine-pyrazolopyridine series of Akt inhibitors and their structural features when bound to PKA are also discussed.
The structure of fluorinated indazoles: The effect of the replacement of a H by a F atom on the supramolecular structure of NH-indazoles
Teichert, Johannes,Oulie, Pascal,Jacob, Kane,Vendier, Laure,Etienne, Michel,Claramunt, Rosa M.,Lopez, Concepcion,Perez Medina, Carlos,Alkorta, Ibon,Elguero, Jose
, p. 936 - 946 (2008/02/12)
The structures of three NH-indazoles (3-methyl, 3-trifluoromethyl and 3-trifluoromethyl-4,5,6,7-tetrafluoroindazoles) have been determined by X-ray crystallography. These three compounds, together with 3-methyl-4,5,6,7- tetrafluoroindazole, whose X-ray st
Synthesis of 1H-indazoles by reductive cyclization of o-nitro-ketoximes
O'Dell, David K.,Nicholas, Kenneth M.
, p. 373 - 382 (2007/10/03)
ortho-Nitro-ketoximes are converted to 1H-indazoles upon reaction with carbon monoxide with [Cp*Fe(CO)2]2 as catalyst.
Fluorinated indazole derivatives and a process for their preparation
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, (2008/06/13)
Compound of the formula: STR1 in which the nucleus A is unsubstituted or substituted by one or two nitro, amino, alkyl, alkoxy, chlorine or bromine and the alkyl and alkoxy each contain up to two carbon atoms and process for the preparation of such compou
