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