Process for the preparation of n-4-¬(substituted...

C - Chemistry – Metallurgy – 07 – D

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C07D 333/24 (2006.01) C07D 307/52 (2006.01) C07D 307/54 (2006.01) C07D 333/20 (2006.01)

Patent

CA 2174548

A process for preparing a compound of structure (I), where A is oxygen and sulfur and R1 is selected from the group consisting of hydrogen, halogen, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, and trifluoromethyl, and R2 is alkyl of one to four carbon atoms, comprising coupling a compound of formula (II), where X is bromine or iodine, with an N- hydroxyurea compound of formula (III), in the presence of a palladium catalyst. The compounds of formula (I) are inhibitors of the enzyme 5- lipoxygenase and are thus useful as therapeutic agents for the treatment of allergic and inflammatory disease conditions.

L'invention concerne un procédé de préparation d'un composé de structure (I), dans laquelle A représente oxygène et soufre et R?1¿ est choisi dans le groupe comprenant hydrogène, halogène, alkyle contenant un à six atomes de carbone, alcoxy contenant un à six atomes de carbone, et trifluorométhyle, et R?2¿ représente alkyle contenant un à quatre atomes de carbone. Ledit procédé consiste à accoupler un composé de formule (II), dans laquelle X représente brome ou iode, avec un composé de N-hydroxyurée de formule (III), en présence d'un catalyseur au palladium. Les composés de formule (I) qui sont des inhibiteurs de l'enzyme 5-lipoxygénase sont utilisés en tant qu'agents thérapeutiques pour le traitement d'états pathologiques allergiques et inflammatoires.

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