| 氨磺必利的合成 |
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| 引用本文： | 程玉红,康江鹏,陈蔚,罗振福,孙波. 氨磺必利的合成[J]. 中国医药工业杂志, 2011, 42(11) |
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| 作者姓名： | 程玉红 康江鹏 陈蔚 罗振福 孙波 |
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| 作者单位： | 1. 天津理工大学化学化工学院,天津,300191
2. 天津药物研究院化学制药部,天津,300193 |
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| 摘 要： | 4-乙酰胺基-2-甲氧基苯甲酸甲酯经浓硫酸磺化、水解、氯化、还原后与溴乙烷反应,再水解得到3-乙基磺酰基-4-氨基-6-甲氧基苯甲酸,最后与1-乙基-2-氨甲基吡咯烷在三乙胺和氯甲酸乙酯作用下缩合制得抗精神分裂症药氨磺必利,总收率约61％.
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| 关 键 词： | 氨磺必利 抗精神分裂症药 合成 |
Synthesis of Amisulpride |
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| CHENG Yuhong,KANG Jiangpeng,CHEN Wei,LUO Zhenfu,SUN Bo. Synthesis of Amisulpride[J]. , 2011, 42(11) |
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| Authors: | CHENG Yuhong KANG Jiangpeng CHEN Wei LUO Zhenfu SUN Bo |
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| Affiliation: | CHENG Yuhong~1,KANG Jiangpeng~(2*),CHEN Wei~2,LUO Zhenfu~2,SUN Bo~1 (1.Dept.of Chemistry and Chemical Engineering,Tianjin University of Technology,Tianjin 300191,2.Centre for Chemical Pharmaceutical Research,Tianjin Institute of Pharmaceutical Research,Tianjin 300193) |
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| Abstract: | Amisulpride,a novel atypical antipsychotic drug,was synthesized from methyl 4-acetamido-2-methoxybenzoate by sulfonation with sulfuric acid,hydrolysis,chlorination,reduction,reaction with bromoethane and then hydrolysis to give 3-ethylsulfonyl-4-amino-6-methoxybenzoic acid,which was subjected to condensation with 1-ethyl-2-(aminomethyl) pyrrolidine in the presence of triethylamine and ethyl chloroformate.The overall yield was about 61%. |
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| Keywords: | amisulpride antipsychotic drug synthesis |
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