Process for preparing aminocrotonylamino-substituted...

Details Process for preparing aminocrotonylamino-substituted... Process for preparing aminocrotonylamino-substituted...

C - Chemistry, Metallurgy

07

D

C07D 239/94 (2006.01) C07D 405/12 (2006.01) C07F 9/6512 (2006.01)

Patent

CA 2639936

The invention relates to an improved process for preparing aminocrotonylamino- substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have the meanings given in the claims, as well as sulphonyl derivatives of formula (XIII) and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.

La présente invention concerne un procédé amélioré de préparation de dérivés quinazoline à substitution aminocrotonylamino de formule générale (I), dans laquelle les groupes Ra, Rb, Rc et Rd sont tels que définis dans les revendications. L~invention concerne également des dérivés sulfonyle de formule (XIII) et leur utilisation en tant que composant de synthèse pour la préparation des quinazolines de formule (I). Les dérivés quinazoline de formule (I) sont des inhibiteurs de la transduction de signal médiée par les tyrosinekinases et le récepteur du facteur de croissance épidermique (EGF-R) ; elles sont donc particulièrement appropriées pour traiter les maladies tumorales.

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