August 5, 2013

CAS databases provide millions of journal article references from more than 10,000 major scientific journals worldwide, patent and patent family references from 63 patent authorities around the world, and other reputable web sources.

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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