Wu En
2010
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Journal
Chinese Journal of Pharmaceuticals
Abstract
Eplivanserin fumarate,a sedative-hypnotic drug was synthesized from N-(2-chloroethyl)dimethyl amine hydrochloride by reaction with acetoxime sodium and then hydrolysis to give the key intermediate O-(2-dimethylaminoethyl)hydroxylamine dihydrochloride(5),which was subjected to condensation with(E)-1-(2-fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one(8) followed by treatment with fumaric acid in 47% overall yield.