摘要 |
<p>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-imidazoÄ4,5-cÜquinoline, of formula (I) <CHEM> 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.</p> |