PREPARATION OF SUBSTITUTED QUINAZOLINES

BARTH HUBERT GANGOLF KLEMENS, BRIDGES ALEXANDER JAMES, HEEMSTRA RONALD JOSEPH, HORNE NICOLE MARCIA, HUGHES ROBERT CRAIG, JACKS THOMAS ELLIOTT, MCNAMARA DENNIS JOSEPH, SCHNEIDER SIMON, STEINER KLAUS IRENAEUS, TOOGOOD PETER LAURENCE, WINTERS ROY THOMAS
2005
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Methods for preparing substituted quinazolines as irreversible tyrosine kinase inhibitors are disclosed, including compounds useful for treating endometriosis and minimizing side products via specific protecting schemes.

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Abstract

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.

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europepmc
last seen: 2026-09-06T09:34:12.023084+00:00