| 摘要 |
Synthesis of deactivated anilines. This process is defined in that it comprises at least one stage consisting in reacting a compound of formula (I): <IMAGE> with: - R1 chosen from the groups whose anions (R1<->) form excellent leaving groups, advantageously from bromine or chlorine atoms, preferably the latter are considered to be a good leaving group, those in which the acid associated with the anion has a pKa value at most equal to 1, advantageously to 0, preferably to -1; - R2 chosen from hydrogen, hydrocarbon chains, halogens, groups which are electron-withdrawing (EWG) advantageously by an inductive but not mesomeric effect; - R3 is of no consequence but it is advantageous that it should be chosen from hydrogen and groups which are at least as withdrawing due to an inductive effect as the alkyl groups; - R4 is chosen from hydrogen, hydrocarbon chains, halogens and groups which are electron-withdrawing advantageously by an inductive but not mesomeric effect; - R5 is of no consequence but it is advantageous that it should be chosen from hydrogen and groups which are at least as withdrawing due to an inductive effect as the alkyl groups; - R6 chosen from hydrocarbon chains, halogens, groups which are electron-withdrawing advantageously by an inductive but not mesomeric effect; with the condition that at least one of the groups R1, R6 and preferably R5 is electron-withdrawing by an inductive effect; it being possible for R2 and R3 and/or R5 and R6 to form at least one ring, optionally aromatic, if appropriate substituted, with a dialkylamide in the presence of a base and at a temperature of between 150 and 300@C, preferably between 180@C and 250@C (in the present description the zero places are not significant unless otherwise stated). Application to organic synthesis. |
