23779-97-7Relevant articles and documents
Design, synthesis and characterization of new 1,2,3-triazolyl pyrazole derivatives as potential antimicrobial agents: Via a Vilsmeier-Haack reaction approach
Bhat, Manjunatha,Nagaraja,Kayarmar, Reshma,Peethamber,Shafeeulla, R. Mohammed
, p. 59375 - 59388 (2016)
The synthesis of a new series of 3-{5-methyl-1-[2-methyl-3-(trifluoromethyl) phenyl/substituted phenyl]-1H-1,2,3-triazol-4-yl}-1-(aryl)-1H-pyrazole-4-carbaldehyde compounds (5a-n) was carried out via a Vilsmeier-Haack formylation of 4-{(1E)-1-[2-(aryl) hydrazinylidene]ethyl}-5-methyl-1-[2-methyl-3-(trifluoromethyl)phenyl/substituted phenyl]-1H-1,2,3-triazole (4a-n) with a phosphorous oxychloride and DMF mixture. The newly synthesized compounds were characterized using IR, 1H NMR, 13C NMR, mass spectral data and elemental analysis. The newly synthesized compounds were screened for their in vitro anti-bacterial, anti-fungal and anti-oxidant activities. Some of the synthesized compounds displayed a broad spectrum of antimicrobial activities and moderate to good anti-oxidant activities. The anti-bacterial results were further supported by in silico molecular docking studies of these compounds for the inhibition of E. coli MurB enzyme (PDB code: 2MBR) and showed a minimum binding energy and good affinity towards the active pocket comparable with the standard drug Ciproflaxin. Thus, they may be considered as good inhibitors of the E. coli MurB enzyme (PDB code: 2MBR).
Coordinating Activation Strategy-Induced Selective C?H Trifluoromethylation of Anilines
Xu, Jun,Cheng, Ke,Shen, Chao,Bai, Renren,Xie, Yuanyuan,Zhang, Pengfei
, p. 965 - 970 (2018/02/12)
A simple protocol for the synthesis of 2-(trifluoromethyl)aniline derivatives through a coordinating activation strategy was developed. The reaction showed good reactivity and gave the target products in moderate to good yields. Pleasingly, the directing group could be recovered in excellent yield. Furthermore, this strategy allowed efficient access to the synthesis of floctafenine. A single-electron-transfer mechanism was proposed to be responsible for this trifluoromethylation reaction.
Process for the preparation of 4-chloroquinolines
-
, (2008/06/13)
Novel process for the preparation of 4-chloroquinolines of the formula STR1 wherein X is in the 5,6,7 or 8-position and is selected from the group consisting of hydrogen, methyl, halogen, CF3 --, CF3 O-- and CF3 S-- by reacting a compound of the formula STR2 or a functional derivative thereof with a chlorination agent in the presence of an oxidation agent and to a novel intermediate.
