Chemagis Ltd.

Dionne Montviliski

Joseph Kaspi

Oded Arad

Vladimir Naddaka

Shady Saeed

Lior Zelikovitch

Shadi Saeed

The present invention provides a process for preparing 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (Imiquimod) of formula (I). The process comprises heating 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (II) with formamide, and optionally with bubbling of gaseous ammonia to afford Imiquimod of formula (I). According to the present invention, by using this process and novel purification methods, essentially as described herein, highly pure Imiquimod is obtained.

Process for preparing Imiquimod

The invention provides a process for preparing 1-methylindazole-3-carboxylic acid of formula (I): which comprises reacting a methylating agent with indazole-3-carboxylic acid of formula (VI): in the presence of an alkaline earth metal oxide or alkoxide in an appropriate solvent. Also provided is a process for producing Granisetron, using the method of the present invention for producing 1-methylindazole-3-carboxylic acid.

Process for preparing 1-methylindazole-3-carboxylic acid

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Givataim, Israel

Dionne Montviliski