106635-86-3Relevant articles and documents
Process for the preparation of anti-malarial drugs
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, (2008/06/13)
The invention relates to novel intermediates and processes for the preparation of quinoline compounds useful as anti-malarial drugs and novel intermediates useful in the process. A process for the preparation of a compound of formula (I) in which R1is C1-6alkyl; R2and R3are independently hydrogen, halogen, trifluoromethyl or C1-6alkoxy; R4is C1-6alkyl; R5is hydrogen or C1-6alkyl; and R6or amino which comprises reacting a compound of formula (II) in which R1, R4and R5are as defined in formula (I) and X is a leading group with a compound of formula (III).
Antimalarials. 16. Synthesis of 2-substituted analogues of 8-[(4-amino-1-methylbutyl)amino]-6-methoxy-4-methyl-5-[3- (trifluoromethyl)phenoxy]quinoline as candidate antimalarials
LaMontagne,Blumbergs,Smith
, p. 1728 - 1732 (2007/10/02)
A series of 2-substituted analogues of the exceptional drug 8-[(4-amino-1-methylbutyl)amino]-6-methoxy-4-methyl-5-[3- (trifluoromethyl)phenoxy]quinoline (I) were prepared and evaluated for both suppressive and prophylactic antimalarial activity. The preparation of analogues of compound I was of interest due to the high level of both blood and tissue schizonticidal activity demonstrated by this compound. One analogue, 8a, was found to be both more active and less toxic than the parent compound I. In addition, three analogues of example 8a were prepared. Although two of the three analogues showed significant antimalarial activity, both were inferior to compound 8a.