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 2230451

A process for producing 1,2,3,4-tetrahydro-2,4-dioxo-quinazoline-1-yl acetic acid derivatives of the formula (I) in which R1, R2, R3 and R4 are mutually independently hydrogen, halogen, OH, NO2, (C1-C6)alkoxy, (C1-C6)alkyl, halogen- substituted (C1-C6)alkyl; R5 is hydrogen, (C1-C6)alkyl, phenyl where the alkyl or phenyl radical may also be substituted by halogen atoms; in which an anthranilic acid derivative of formula (II), in which R1 to R5 have the above meanings and R6 is hydrogen, (C1-C6)alkyl or phenyl, where the alkyl or phenyl radical may also be substituted by halogen atoms, is reacted with a metal cyanate and hydrogen chloride in the presence of an inert solvent.

L'invention concerne la production de dérivés d'acide acétique 1,2,3,4-tétrahydro-2,4-dioxo-quinazolin-1-yle de la formule (I) où R?1¿, R?2¿, R?3¿, R?4¿ représentent indépendamment les uns des autres hydrogène, halogène, OH, NO¿2?, alcoxy (C¿1?-C¿6?), alkyle (C¿1?-C¿6?), alkyle (C¿1?-C¿6?) substitué par halogène. R?5¿ représente hydrogène, alkyle (C¿1?-C¿6?), phényle. Le reste alkyle ou le reste phényle peuvent également être substitués par des atomes d'halogène. On obtient ces dérivés en faisant réagir un dérivé d'acide anthramilique de la formule (II) où R¿1? à R¿5? ont la signification susmentionnée et où R?6¿ représente hydrogène, alkyle (C¿1?-C¿6?) ou phényle, les restes d'alkyle ou de phényle pouvant également être substitués par des atomes d'halogène, avec un cyanate métallique et de du gaz chlorhydrique en présence d'un solvant inerte.

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