| 摘要 |
A process for the preparation of Imiquimod and novel hydroxylamino and hydrazine derivatives, useful as intermediates in its preparation. The process includes the reaction of 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline, of formula (I) with a compound of formula (II) <?in-line-formulae description="In-line Formulae" end="lead"?>NH<SUB>2</SUB>-X (II) <?in-line-formulae description="In-line Formulae" end="tail"?> wherein X is an -OR or -NR<SUB>1</SUB>R<SUB>2 </SUB>group, in which R is hydrogen, a C<SUB>1</SUB>-C<SUB>6 </SUB>alkyl, aryl-C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl, aryl or -SO<SUB>3</SUB>H (sulfonic) group; and each of R<SUB>1 </SUB>and R<SUB>2 </SUB>is independently hydrogen, a C<SUB>1</SUB>-C<SUB>6 </SUB>alkyl, aryl-C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl, aryl or -SO<SUB>2</SUB>R<SUB>3 </SUB>group, in which R<SUB>3 </SUB>is an aryl group and, if necessary, the reaction with a reducing agent.
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