23779-94-4Relevant articles and documents
Synthetic method of 8-(trifluoromethyl)quinoline-3-carboxylate
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Paragraph 0062; 0068-0070, (2018/09/11)
The invention provides a synthetic method of 8-(trifluoromethyl)quinoline-3-carboxylate. The synthetic method comprises the following steps: reacting 2-(trifluoromethyl)aniline serving as a starting raw material to obtain 8-(trifluoromethyl)quinoline-3-ethyl ester carboxylate; lastly, hydrolyzing the 8-(trifluoromethyl)quinoline-3-ethyl ester carboxylate in an alkaline environment to obtain 8-(trifluoromethyl)quinoline-3-carboxylate. According to the synthetic method of the 8-(trifluoromethyl)quinoline-3-carboxylate provided by the invention, a synthetic route taking 2-(trifluoromethyl)anilineas a raw material is provided. The synthetic method has the advantages of simple synthetic route, reasonable process selection, low raw material cost, adoption of simple and readily-available raw materials, convenience in operation and post-treatment, high total yield, no use of any highly-toxic reagent, easiness in amplification, realization of large-scale production and the like.
Design and regioselective synthesis of trifluoromethylquinolone derivatives as potent antimicrobial agents
Garudachari,Isloor, Arun M.,Satyanarayana,Fun, Hoong-Kun,Pavithra,Kulal, Ananda
, p. 422 - 432 (2013/10/01)
Three series of new trifluoromethyl substituted quinolone derivatives were synthesized (4a-f, 6a-f and 8a-f) from corresponding substituted anilines by multi-step reactions. The regioselective alkylation with different alkyl halides were carried out by approaching two different routes to get the final products in good yield. Newly synthesized compounds were characterized by spectral study and also by C, H, N analyses. Three dimensional structure of 2b and 4b were also confirmed by single crystal X-ray studies. The final compounds (4a-f, 6a-f and 8a-f) were screened for their in-vitro antibacterial and antifungal activity by well plate method (zone of inhibition). The results revealed that, compounds 4a, 6b, 6c and 8e showed significant antibacterial activity as compared to the standard drug Ciprofloxacin. The compound 8a was found to be a potent antifungal agent.
Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents
Eswaran, Sumesh,Adhikari, Airody Vasudeva,Pal, Nishith K.,Chowdhury, Imran H.
supporting information; experimental part, p. 1040 - 1044 (2010/06/14)
A series of 26 new quinoline derivatives carrying active pharmacophores has been synthesized and evaluated for their in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB), Mycobacterium smegmatis (MC2), and Mycobacterium fortuitum following the broth micro dilution assay method. Compounds 13e, 13i, 13k, 14a, 14c, 14i, and 14k exhibited significant minimum inhibition concentrations, when compared with first line drugs isoniazid (INH) and rifampicin (RIF) and could be ideally suited for further modifications to obtain more efficacious compounds in the fight against multi-drug resistant tuberculosis.