Method for the production of amino crotonyl compounds

C - Chemistry – Metallurgy – 07 – D

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C07D 405/12 (2006.01)

Patent

CA 2541928

The invention relates to an improved method for the production of 4-[(3-chloro- 4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-butene-1-yl]amino}-7- ((S)-tetrahydrofurane-3-yloxy)-quinazoline and related amino crotonyl compounds. The invention also relates to a suitable salt of 4-[(3-chloro-4- fluorphenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-butene-1-yl]amino}-7-((S)- tetrahydrofurane-3-yloxy)-quinazoline for use as an active ingredient for a medicament.

L'invention concerne un procédé amélioré de production de 4-[(3-chloro-4-fluorophényl)amino]-6-{[4-(N,N-diméthylamino)-1-oxo-2-butén-1-yl]amino}-7-((<I>S</I>)-tétrahydrofuran-3-yloxy)-quinazoline et de composés aminocrotonyliques apparentés, ainsi que la production d'un sel adapté de 4-[(3-chloro-4-fluorophényl)amino]-6-{[4-(N,N-diméthylamino)-1-oxo-2-butén-1-yl]amino}-7-((<I>S</I>)-tétrahydrofuran-3-yloxy)-quinazoline destiné à être utilisé comme principe actif pharmaceutique.

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