Progress toward the synthesis of N-Methyl Improgan

Monika Siepsiak

Abstract


Improgan is a synthetic drug that appears to be a powerful pain reliever without the addictive properties of opiate drugs. To date, improgan has only been administered through direct injections into the brain of laboratory animals due to the fact that it does not cross the blood-brain barrier. The goal of this research is to synthesize N-methyl improgan, a potentially brain penetrating analogue. Replacing the N-H on the imidazole ring of improgan with an N-methyl group will decrease the amount of hydrogen bond donors as well as the polarity of the compound, potentially allowing it to cross the blood-brain barrier. A seven-step synthesis has been proposed in order to construct this chemical congener. The progress towards the synthesis of N-methyl improgan will be described in detail. The synthesis produces isomers with methylation occurring at the τ(N-1) or π(N-3) position. Different routes and conditions used to alter the ratio of the two isomers will be discussed as well as the separation of these isomers.

 


Keywords


Improgran; N-Methylation; Synthesis

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