Preparation of substituted quinazolines

Details Preparation of substituted quinazolines Preparation of substituted quinazolines

C - Chemistry, Metallurgy

07

D

C07D 239/94 (2006.01)

Patent

CA 2514933

Methods and materials for preparing irreversible inhibitors of tyrosine kinases of general Formula (1) are disclosed. Such inhibitors, which include N- [4-)3-chloro-4-floro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6- yl]-acrylamide, are useful for treating cancer, retenosis, atherosclerosis, endometriosis and psoriasis. The disclosed methods employ protecting schemes to minimize undesirable diacryloylamino-quinazoline side products.

L'invention concerne des procédés et du matériel pour la préparation d'inhibiteurs irréversibles de tyrosine kinases représentés par la formule générale 1. Lesdits inhibiteurs, qui comprennent N-[4-(3-chloro-4-floro-phénylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, sont utiles pour le traitement du cancer, de la resténose, de l'athérosclérose, de l'endométriose et du psoriasis. Les procédés de l'invention consistent à utiliser des schémas de protection pour minimiser les produits secondaires indésirables de la diacryloylamino-quinazoline.

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