- Synthesis of Zopiclone
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(CAS NO.: ), with its systematic name of 4-Methyl-1-piperazinecarboxylic acid ester with 6-(5-chloro-2-pyridyl)-6,7-dihydro-7-hydroxy-5H-pyrrolo(3,4-b)pyrazin-5-one , could be produced through many synthetic methods.
Following is one of the reaction routes: Pyrazine-2,3-dicarboxylic (I) could react with 2-amino-5-chloropyridine (II) to produce 3-(5-chloro-2-pyridyl)carbamoyl pyrazine-2-carboxylic acid (III) in refluxing acetonitrile, and then the compound is cyclized by treatment with refluxing SOCl2 giving 6-(5-chloropyrid-2-yl)-5,7-dioxo-5,6-dihydropyrrolo[3,4-b]pyrazine (IV). The partial reduction of (IV) with KBH4 in dioxane-water produces 6-(5-chloro-2-pyridyl)-7-hydroxy-5,6-dihydropyrrolo[3,4-b]pyrazin-5-one (V), which is finally esterified with 4-methylpiperazine-1-carbonyl chloride (VI) by means of NaH in DMF.


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