Patent ID: 6664390
Filing Date: 2003-12-16
Classification: C07D

Abstract:
Process for the preparation of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitroquinazolin-4-yl]-amine (1) 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) then 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 optionally hydrogenates (I) directly in the reaction solution to give (III).