METHOD FOR SIMPLIFIED PRODUCTION OF (3-CHLORO-4-FLUORO-PHENYL)-7-(3-MORPHOLINO-4-YL-PROPOXY)-6-NITRO-QUINAZOLINE-4-YL-AMINE OR (3-CHLORO-4-FLUORO-PHENYL)-7-(3-MORPHOLINO-4-YL-PROPOXY)-6-AMINO-QUINAZOLINE-4-YL-AMINE

摘要

1. Process for the preparation of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitroquinazolin-4-yl]-amine (I) or of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-aminoquinazolin-4-yl]-amine (VII) characterised in that, in a one-pot reaction, in 3 or 4 reaction steps, one first reacts 7-fluoro-6-nitroquinazolin-4(3H)-one (III) with thionyl chloride to give 4-chloro-7-fluoro-6-nitroquinazoline (IV) reacts this with 3-chloro-4-fluoroaniline to give 4-(3-chloro-4-fluoroanilino)-7-fluoro-6-nitroquinazoline (V) and subsequently with 3-morpholin-4-yl-propan-1-ol (VI) to give (I) and possibly hydrogenates (I) directly in the reaction solution to give (III).