【摘要】 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%。更多还原

【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.更多还原