A process for the preparation of imiquimod

Details A process for the preparation of imiquimod A process for the preparation of imiquimod

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01)

Patent

CA 2510576

A process for the preparation of Imiquimod and novel hydroxylamino and hydrazine derivatives, useful as intermediates in its preparation. The process comprises the reaction of 4-chloro-1-isobutyl-1H- imidazo[4,5-c]quinoline, of formula (I) Image with a compound of formula (II) NH2-X (II) wherein X is an -OR or -NR1R2 group, in which R is hydrogen, a C1-C6 alkyl, aryl-C1-C4 alkyl, aryl or -SO3H (sulfonic) group; and each of R1 and R2 is independently hydrogen, a C1-C6 alkyl, aryl-C1-C4 alkyl, aryl or -SO2R3 group, in which R3 is an aryl group and, if necessary, the reaction with a reducing agent.

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