18706-25-7Relevant articles and documents
Preparation method of quinolone derivate
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Paragraph 0020; 0021; 0022, (2018/07/30)
The invention discloses a preparation method of a quinolone derivate 1-(2-(trifluoromethyl) quinolone-4-gruop) ethylamine. The method is characterized in that 2-(trifluoromethyl) quinolone-4-alcohol is used as the initial raw material and is subjected to bromination, cyaniding, grignard reaction and amination reduction to obtain a target product. The compound is an important intermediate of a medicine.
Selective and efficient structural elaboration of 2-(trifluoromethyl)quinolinones
Marull, Marc,Schlosser, Manfred
, p. 1576 - 1588 (2007/10/03)
The acid-catalyzed cyclization-condensation between anilines and ethyl 4,4,4-trifluoroacetoacetate affords 1,4-dihydro-2-trifluoromethyl-4H-4-quinolinones (1), which can easily be converted into 4-bromo-2-(trifluoromethyl)quinolines. These undergo halogen/metal exchange, generating 2-trifluoromethyl-4-quinolyllithiums, when treated with butyllithium, and hydrogen/metal exchange, generating 4-bromo-2-trifluoromethyl-3-quinolyllithiums, when treated with lithium diisopropylamide. Trapping of the latter intermediates provides 3-functionalized products that may be further elaborated by electrophilic substitution of the bromine atom. A few unexpected findings resulted from these investigations, the most noteworthy being an unprecedented buttressing effect and a counterintuitive halogen reactivity. ( Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003).