| 半富马酸喹硫平的合成研究 |
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| 引用本文： | 梁伟周,刘涛,陈延蕾,陈新志. 半富马酸喹硫平的合成研究[J]. 中国医药工业杂志, 2004, 35(12): 705-707 |
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| 作者姓名： | 梁伟周 刘涛 陈延蕾 陈新志 |
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| 作者单位： | 浙江大学材料与化工学院,浙江,杭州,310027 |
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| 摘 要： | 2-氨基二苯硫醚和三光气反应得到的2-异氰酸基二苯硫醚在多聚磷酸中闭环后,经氯代、与哌嗪缩合得到11-哌嗪-1-基二苯并[b,f][1,4]硫氮杂革,由2-(2-氯乙氧基)乙醇进行哌嗪N4-位烷基化反应后与富马酸成盐,制得抗精神病药半富马酸喹硫平,总收率63.4%(以2-氨基二苯硫醚计).
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| 关 键 词： | 喹硫平 抗精神病药 合成 |
| 文章编号： | 1001-8255(2004)12-0705-03 |
Synthesis of Quetiapine Hemifumarate |
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| LIANGWei-Zhou,LIU Tao,CHENYan-Lei,CHEN Xin-Zhi. Synthesis of Quetiapine Hemifumarate[J]. , 2004, 35(12): 705-707 |
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| Authors: | LIANGWei-Zhou LIU Tao CHENYan-Lei CHEN Xin-Zhi |
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| Affiliation: | LIANGWei-Zhou,LIU Tao,CHENYan-Lei,CHEN Xin-Zhi* |
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| Abstract: | Quetiapine hemifumarate wassynthesized in 63.4% overall yield from 2-aminodiphenyl sulfide and triphosgene to give 2-isocyanato diphenyl sulfide, which subjected to cyclization in polyphosphoric acid, chlorination and condensation with piperazine to afford 11-piperazin-1-yl-dibenzo[b,f][1,4]thiazepine followed by N4-alkylation of piperazine and then salification with fumaric acid. |
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| Keywords: | quetiapine antipsychotic synthesis |
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