PREPARATION OF SUBSTITUTED QUINAZOLINES

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, restenosis, atherosclerosis...

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Bibliographische Detailangaben
Hauptverfasser: HEEMSTRA, RONALD JOSEPH, BARTH, HUBERT GANGOLF KLEMENS, STEINER, KLAUS IRENAUS, MCNAMARA, DENNIS JOSEPH, WINTERS, ROY THOMAS, JACKS, THOMAS ELLIOTT, TOOGOOD, PETER LAURENCE, HORNE, NICOLE MARCIA, HUGHES, ROBERT CRAIG, BRIDGES, ALEXANDER JAMES, SCHNEIDER, SIMON
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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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, restenosis, atherosclerosis, endometriosis and psoriasis. The disclosed methods employ protecting schemes to minimize undesirable diacryloylamino-quinazoline side products.