PREPARATION OF SUBSTITUTED QUINAZOLINES

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, ath...

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1. Verfasser: THOMAS ELLIOTT JACKS
Format: Patent
Sprache:eng ; spa
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Zusammenfassung: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. Se describen metodos y materiales para la preparacion de inhibidores irreversibles de tirosina quinasas de Formula general 1. Dichos Inhibidores, que incluyen N-[4 -(3- cloro- 4-fluoro- fenilamino)- 7-(3-morfolin -4-il- propoxi)- quinazolin -6-il] -acrilamida, son utiles para el tratamiento del cancer, restenosis, ateroesclerosis, endometriosis y psoriasis. Los metodos descritos emplean estrategias protectoras para minimizar productos laterales diacriloilamino-quinazolina indeseables. (ver formula 1).