| abstract |
IT REFERS TO A PROCEDURE FOR THE PREPARATION OF QUINAZOLINES SUBSTITUTED FOR FORMULA I, AMONG OTHERS, INCLUDING ITS SALT, ESTER, AMIDA WHERE R1, R2 AND R3 ARE H, HALOGEN, NO2, CN, CF3, AMONG OTHERS; R4 AND R6 ARE H, HYDROXY, HALOGEN, C1-C4 ALKYL, AMONG OTHERS; R5 IS PHENYL, PYRIDYL, FURIL, THIAZOLIL, AMONG OTHERS; Z IS H, HALOGEN, C1-C6, C3-C8 CYCLOALKYL, AMONG OTHERS, WITH THE CONDITION THAT WHEN Z IS MONOVALENT, R5 IS ABSENT. THIS METHOD INCLUDES REMOVING THE PROTECTIVE GROUP G OF A COMPOUND OF FORMULA 10 TO GIVE A COMPOUND OF FORMULA 1. THE PREFERRED COMPOUNDS ARE: (3-CHLORO-4-FLUORO-PHENYL) - (3,4-DIMETOXY-BENZYL) - (7 -FLUORO-6-NITROQUINAZOLIN-4-IL) -AMINE; (3-CHLORO-4-FLUORO-PHENYL) - (3,4-DIMETOXY-BENZYL) - [7- (3-MORPHOLIN-4-IL-PROPOXY) -6-NITROQUINAZOLIN-4-IL] -AMINE; N4- (3-CHLORO-4-FLUORO-PHENYL) -N4- (3,4-DIMETOXY-BENZYL) -7- (3-MORPHOLIN-4-IL-PROPOXY) -QUINAZOLIN-4,6-DIAMINE; AMONG OTHERS. THESE COMPOUNDS ARE IRREVERSIBLE INHIBITORS OF TYROSINE KINASE AND ARE USEFUL TO TREAT CANCER, RESTENOSIS, ATHEROSCLEROSIS, ENDOMETRIOSIS AND PSORIASIS |