Patent ID: 7659398
Filing Date: 2010-02-09
Classification: C07D

Abstract:
1. A process for preparing 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (I) (imiquimod): the process comprising: heating a mixture comprising 4-chloro-1-isobutyl-1H-imidazo[4,5-c]-quinoline of formula (II):  and ammonia in a polar, aprotic solvent, which is dimethyl sulfoxide (DMSO), N-methyl-2-pyrrolidone (NMP), tetramethylene sulfone (sulfolane), hexamethylphosphorotriamide (HMPA), or a mixture thereof, at relatively moderate pressure, to produce the compound of formula (I); cooling the reaction mixture; isolating the compound of formula (I); and optionally purifying the compound of formula (I).