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