Process for producing quinazoline derivatives

Details Process for producing quinazoline derivatives Process for producing quinazoline derivatives

C - Chemistry, Metallurgy

07

D

C07D 239/96 (2006.01)

Patent

CA 2283514

A process for producing quinazoline derivatives of general formula (I) or salts thereof on an industrial scale, wherein R1 represents hydrogen or halogen; R2 represents carboxyl or protected carboxyl; and A represents lower alkylene, by reacting a compound of the general formula (II): C1-A-R2, wherein R1 is as defined above, or a salt thereof with a silylating agent and then with a compound of general formula (III), wherein R1 and A are each as defined above, or a salt thereof and, if necessary, desilylating the product.

L'invention concerne un procédé de production à l'échelle industrielle de dérivés de quinazoline de formule générale (I) ou des sels de ceux-ci. Dans ladite formule (I), R?1¿ représente hydrogène ou halogène; R?2¿ représente carboxyle ou carboxyle protégé; et A représente alkylène inférieur. Ledit procédé consiste à faire réagir un composé de formule générale (II), dans laquelle R?1¿ est tel que défini ci-avant, ou un sel de celui-ci, avec un agent de silylation et ensuite avec un composé de formule générale (III), dans laquelle R?1¿ et A sont tels que défini ci-avant, ou un sel de celui-ci, et si nécessaire, à désilyler ledit produit.

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