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半富马酸喹硫平的合成 被引量:8

Synthesis of quetiapine hemifumarate
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摘要 以邻氯硝基苯和硫代水杨酸为起始原料,水相中碱化缩合成2-硝基2'-羧基二苯硫醚(2)后,通过铁粉还原成2-氨基2-'羧基二苯硫醚(3),经PPA催化环合制得10H-二苯并[b,f][1,4]硫氮杂卓-11-酮(4),再通过产物4与三氯氧磷氯化、与哌嗪缩合、与侧链2-(2-氯乙氧基)乙醇(6)缩合成得喹硫平(5),最后在乙醇中成盐合成得半富马酸喹硫平(1),总收率47.60%,结构经IR和1 H NMR确认. The synthetic routes had been studied for 10H-dibenzothiazepine-11-ketone(4),which was synthesized using thiosalicylic acid and o-chloro-nitrobenzene as starting materials,2-amino-2'-carboxyl diphenylsulfide(2) was synthesized in aqueous phase,which was reduced by iron powder and cyclized in the polyphosphoric acid.Quetiapine Hemifumarate(1) was produced from 4,in the process of chlorination with phosphorus oxychloride,condensed with piperazine and 2-amino-4-chloro-pyrimidine(6),salt formed with fumaric acid in ethyl alcohol.The total yield was 47.60%.The structrue was confirmed by IR and 1H NMR.
出处 《武汉工程大学学报》 CAS 2011年第10期13-16,共4页 Journal of Wuhan Institute of Technology
关键词 抗精神病药 半富马酸喹硫平 合成工艺 antipsychotic drug quetiapine hemifumarate synthesis study
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