99199-60-7Relevant articles and documents
Synthesis of novel of 2, 5-disubstituted 1, 3, 4- oxadiazole derivatives and their in vitro anti-inflammatory, anti-oxidant evaluation, and molecular docking study
Dongare, Balasaheb B.,Ghanwat, Anil A.,Kashid, Bharat B.,Khedkar, Vijay M.,More, Kishor R.,Salunkhe, Pravin H.
, (2020/04/15)
A series of novel 2, 5-disubstituted 1, 3, 4-Oxadiazole derivatives as a potential anti-inflammatory, and anti-oxidant agent were synthesized via cyclisation. Hydrazide molecule treated with substituted acids in the presence of phosphorus oxychloride (POCl3) as an efficient reagent as well as solvent by conventional method with shorter reaction time and excellent yield. The newly synthesized 1, 3, 4- oxadiazole derivatives exhibited excellent to good anti-inflammatory and anti-oxidant activities compaired to the standard drugs. Molecular docking study on the crucial anti-inflammatory target–cyclooxygenase-2 (COX-2) revealed the ability of the scaffold to correctly recognize the active site and achieve significant bonded and non-bonded interactions with key residues therein. This study could identify potential compounds which can be pertinent starting points for structure-based drug design to obtain newer anti-inflammatory agents.
6-fluoro-chroman-2-carboxylic acid
-
, (2017/02/17)
The invention discloses a preparation method of 6- fluorochroman-2-formic acid. The method comprises the following steps: with p-fluorophenol and dimethyl acetylenedicarboxylate as initial raw materials, carrying out an addition reaction on p-fluorophenol and dimethyl acetylenedicarboxylate to generate dimethyl 2-(p-fluorophenoxy) acetylenedicarboxylate, hydrolyzing under an alkaline condition to generate 2-(p-fluorophenoxy) butenedioic acid, dissolving obtained 2-(p-fluorophenoxy) butenedioic acid in concentrated sulfuric acid to perform cyclization to generate 6-fluoro-4-oxo-4H-1-benzopyran-2-formic acid, and finally, carrying out pressurized hydrogenation catalytic reduction to obtain 6-fluorochroman-2-formic acid. The method disclosed by the invention has the advantages of simple operation, low cost and high product yield, and reactions in the steps are safe and environment-friendly, so that the method is especially suitable for industrial production.
A mild synthesis of α,α′-[iminobismethylene]bis[6-fluoro- 3,4-dihydro-2H-1 -benzopyran-2-methanol]
Bai, Yihui,Chen, Xinzhi
, p. 807 - 808 (2007/10/03)
A new synthesis of α,α′-[iminobismethylene]bis[6-fluoro- 3,4-dihydro-2H-1-benzopyran-2-methanol (1) is described, with most reactions being carried out at room temperature and normal pressure, that will further contribute to the development of new scalable synthesis of the related drug substance of Nebivolol (overall yield: 33%).
