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[1]明娟,杨艺虹*,张珩,等.半富马酸喹硫平的合成[J].武汉工程大学学报,2011,(10):13-16.
　MING Juan,YANG Yi hong,ZHANG Heng,et al.Synthesis of quetiapine hemifumarate[J].Journal of Wuhan Institute of Technology,2011,(10):13-16.
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《武汉工程大学学报》[ISSN:1674-2869/CN:42-1779/TQ]

卷:
期数:
2011年10期
页码:
13-16
栏目:
化学与化学工程
出版日期:
2011-11-30

文章信息/Info

Title:
Synthesis of quetiapine hemifumarate
文章编号:
16742869(2011)100001304
作者:
明娟; 杨艺虹*; 张珩; 张国龙
武汉工程大学绿色化工过程省部共建教育部重点实验室，湖北 武汉 430074
Author(s):
MING Juan; YANG Yihong; ZHANG Heng; ZHANG Guolong
Key Laboratory for Green Chemical Process of Ministry of Eduction,Wuhan Institute of Technology,Wuhan 430074,China
关键词:
抗精神病药; 半富马酸喹硫平; 合成工艺
Keywords:
antipsychotic drug; quetiapine hemifumarate; synthesis study
分类号:
TQ177.5
DOI:
-
文献标志码:
AAdoi:10.3969/j.issn.16742869.2011.10.004
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1H NMR确认.
Abstract:
The synthetic routes had been studied for 10Hdibenzo［b,f］［1,4］thiazepine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.

参考文献/References:

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［6］Bozsing D,Kovanying L G,Simig G,et al.A process for the preparation of quetiapine and intermediates therefore:WO,2001055125［P］.20010802.
［7］梁伟周,刘涛,陈延蕾,等.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706.
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