A PROCESS FOR THE PREPARATION OF SUBSTANTIALLY PURE 4-AMINO-1-ISOBUTYL-1H-IMIDAZO[4,5-C]-QUINOLINE (IMIQUIMOD)
A process for preparation of Imiquimod comprising oxidation of 1-Isobutyl-1H-imidazo-[4,5-c]-quinoline (II) afforded 1-Isobutyl-1H- imidazo-[4,5-c]-quinoline-5-N-oxide(III) which is isolated in pure form as its hydrochloride salt (IV) followed by conversion to 4-chloro derivative(V) and conversion to corresponding 4-iodo derivative (VI) which is a novel intermediate. This novel intermediate is converted to imiquimod (VIII) and purified via its organic salt. The invention also relates to crystalline polymorphic forms of Imiquimod Maleate, Fumarate and Oxalate.
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(2008/06/13)
A PROCESS FOR PREPARATION OF 4-AMINO-1-ISOBUTYL-1H-IMIDAZO[4,5-C]-QUINOLINE (IMIQUIMOD)
A process for preparation of imiquimod comprising oxidation of 1-Isobutyl-1H-imidazo quinoline quinoline (II) afforded 1-Isobutyl-lH- imidazo-[4,5-c]-quinoline-5-N-oxide (III) which is isolated in pure form as its hydrochloride salt (IV) followed by conversion to 4-chloro derivative(V) and conversion to corresponding 4-iodo derivative (VI) which is a new intermediate. This new intermediate is convened to imiquimod (VIII) and purified via its novel maleate salt.
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(2008/06/13)
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