PROCESS FOR PREPARING 4,6-BIS (ARYLOXY) PYRIMIDINE DERIVATIVES

摘要

Process for preparing 4,6-bis(aryloxy)pyrimidine derivatives A process is provided for preparing 4,6-bis(aryloxy)pyrimidine derivatives. The process is conducted in water as reaction medium and catalyzed by one or more tertiary-amine catalyst(s). It has been found that a water based reaction substantially free of organic solvents can be carried out providing excellent yields by the addition of one or more tertiary-amine catalysts to the reaction medium. This provides a clean reaction and produces the desired product in high yields.

主权项

1. A process for preparing a compound of general formula (I) which comprises either: a) reacting a compound of general formula (II) with an alcohol of the general formula R6-OH, or a salt thereof,i) in the presence of between 0.05 and 40 mol % of one or more tertiary-amine catalyst(s); andii) using water as reaction medium and wherein the reaction medium contains less than 10 w/w % of organic solvent;
or b) reacting a compound of general formula (III) with a compound of general formula (IV) or a salt thereof,i) in the presence of between 0.05 and 40 mol % of one or more tertiary-amine catalyst(s); andii) using water as reaction medium and wherein the reaction medium contains less than 10 w/w % of organic solvent;
wherein:LG represents a leaving group;R1, R2, R3 and R4 represent, independently of one another, hydrogen, halogen, cyano, nitro, alkylcarbonyl, formyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, or optionally halogen-substituted alkyl, aryl, alkoxy, alkylthio, alkylsulphinyl or alkylsulphonyl;R5 is hydrogen, halogen, cyano, nitro, alkylcarbonyl, formyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, or optionally halogen-substituted alkyl, aryl, alkoxy, alkylthio, alkylsulphinyl or alkylsulponyl, or one of the following radicals: wherein * denotes the point of attachment to the phenyl radical of formula (I);
R6 is substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclyl, or a salt thereof;R7 is hydrogen, fluorine, chlorine or bromine; with the proviso that R6 and the radical: are different from each other.