CAJ | 학술논문

N-(2-氯乙基)二甲胺盐酸盐和丙酮肟钠反应后水解制得O-(2-二甲胺基乙基)羟胺二盐酸盐(5);另用邻氟苯乙酮和对羟基苯甲醛经缩合得到(E)-1-(2-氟苯基)-3-(4-羟基苯基)-2-丙烯-1-酮(8).5和8缩合得到的依利色林与富马酸成盐,制得镇静催眠药富马酸依利色林,总收率约47%.
N-(2-록을기)이갑알염산염화병동우납반응후수해제득O-(2-이갑알기을기)간알이염산염(5);령용린불분을동화대간기분갑철경축합득도(E)-1-(2-불분기)-3-(4-간기분기)-2-병희-1-동(8).5화8축합득도적의리색림여부마산성염,제득진정최면약부마산의리색림,총수솔약47%.
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.