August 5, 2013

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The following patent record is from the CAplusSM database.


Patent Number: US 8450482
Title: Process for preparation of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-[[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy]quinazoline
Inventor(s): Boardman, Kay Alison; Cunningham, Oliver Robert; Goundry, William; Laffan, David Dermot Patrick
Patent Assignee(s): AstraZeneca AB, Swed.; AstraZeneca UK Limited
Source: PCT Int. Appl., 46 pp. CODEN: PIXXD2
Language: English

The present invention pertains to a process for the prepn. of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-[[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy]quinazoline and salts thereof.  For example, 2-[4-(4-amino-5-cyano-2-methoxyphenoxy)piperidin-1-yl]-N-methylacetamide (prepn. given) was reacted with N,N-dimethylformamide di-Me acetal in 2-methyltetrahydrofuran in the presence of acetic acid at 76 °C for 16 h to afford 2-[4-[5-cyano-4-[[(dimethylamino)methylene]amino]-2-methoxyphenoxy]piperidin-1-yl]-N-methylacetamide.  The intermediate obtained above was reacted with 3-chloro-2-fluoroaniline in methoxybenzene in the presence of acetic acid at 90°C for 20 h to give the title compd. as the final product.  Pharmaceutical formulations contg. the title compd. as an active ingredient were also disclosed in the present invention.

Please note:  Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention.

 View the full-text here.

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