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US 6,664,390 B2Granted
Method for the simplified production of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitro-quinazoline-4-yl]-amine or (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-amino-quinazoline-4-yl]-amine
AssigneeWarner-Lambert Company
InventorsHubert Barth, Klaus Steiner, Simon Schneider
Life of this patent
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Abstract
The invention concerns a one-pot reaction 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-morpholino-4-yl-propoxy)-6-aminoquinazolin-4-yl]-amine (VII)
Claims1
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).
3 more elements
Dependencies are inferred from the claim text.