Sun Huaf
2015
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Journal
Chinese Journal of Pharmaceuticals
Abstract
Methylnaltrexone bromide was synthesized from naltrexone hydrochloride via condensation with ethylene glycol,etherification with t-butyldimethylchlorosilane and methylation with methyl iodide to give(R)-3-[(tbutyldimethylsilyl) oxy]-17-cyclopropylmethyl-4,5a-epoxy-14-hydroxy-6-(1,3-dioxolane-2-yl)-N-methylmorphinanium iodide,which was subjected to hydrolysis with hydrobromic acid,ion exchange with bromide anion exchange resin.The overall yield was about 53%and HPLC purity was more than 99%.