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US 2003/0158408 A1Published application
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) 1 or of (3-chloro-4-fluorophenyl)-[7-(3-morpholino-4-yl-propoxy)-6-aminoquinazolin-4-yl]-amine (VII) 2
Claims1
Process for the preparation of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitroquinazolin-4-yl]-amine (I)
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- or of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-aminoquinazolin-4-yl]-amine (VII)
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- 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)
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- with thionyl chloride to give 4-chloro-7-fluoro-6-nitroquinazoline (IV)
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- then reacts this with 3-chloro-4-fluoroaniline to give 4-(3-chloro-4-fluoroanilino)-7-fluoro-6-nitroquinazoline (V)
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- and subsequently with 3-morpholin-4-yl-propan-1-ol (VI)
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- to give (I) and possibly hydrogenates (I) directly in the reaction solution to give (III).
9 more elements
Dependencies are inferred from the claim text.