Process for the preparation of anti-malarial drugs

Details Process for the preparation of anti-malarial drugs Process for the preparation of anti-malarial drugs

C - Chemistry, Metallurgy

07

D

C07D 215/22 (2006.01) C07D 215/227 (2006.01) C07D 215/40 (2006.01)

Patent

CA 2231633

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 R1 is C1-5 alkyl; R2 and R3 are independently hydrogen, halogen, trifluoromethyl or C1-5 alkoxy; R4 is C1-6 alkyl; R5 is hydrogen or C1-6 alkyl; and R6 is nitro or amino which comprises reacting a compound of formula (II) in which R1, R4 and R5 are as defined in formula (I) and X is a leading group with a compound of formula (III).

Cette invention concerne de nouveaux produits intermédiaires et des procédés de préparation de composés de quinoline utiles en qualité de médicaments anti-paludiques, ainsi que de nouveaux produits intermédiaires utilisés dans ce procédé. Cette invention concerne un procédé de préparation d'un composé de formule (I) où R<1> représente alkyle C1-6; R<2> et R<3> représentent indépendamment hydrogène, halogène, trifluorométhyle ou alcoxy C1-6; R<4> représente alkyle C1-6; R<5> représente hydrogène ou alkyle C1-6; et R<6> représente nitro ou amino. Ce procédé consiste à faire réagir un composé de formule (II) où R<1>, R<4> et R<5> sont tels que définis dans la formule (I) et X est un groupe partant, avec un composé de formule (III).

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