| 琥珀酸索非那新的合成 |
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| 引用本文： | 李强,朱金林,黄伟,岑均达.琥珀酸索非那新的合成[J].中国医药工业杂志,2012,43(1):1-4. |
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| 作者姓名： | 李强 朱金林 黄伟 岑均达 |
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| 作者单位： | 1. 中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海200437
2. 浙江医药股份有限公司,浙江新昌,312500 |
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| 基金项目： | 国家“重大新药创制”科研重大专项(2009ZX09301-007) |
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| 摘 要： | 苯乙胺依次经酰化、Bischler-Napieralski环合、硼氢化钠还原及拆分制得(S)-1-苯基-1,2,3,4-四氢异喹啉(6),再依次与氯甲酸乙酯缩合,(R)-3-奎宁环醇发生酯交换反应,最后成盐制得膀胱过动症治疗药琥珀酸索非那新,总收率约21％.
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| 关 键 词： | 索非那新 膀胱过度活动症 合成 |
Synthesis of Solifenacin Succinate |
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| Authors: | LI Qiang ZHU Jinlin HUANG Wei CEN Junda |
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| Institution: | 1*(1.Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,State Key Lab.of New Drug & Pharmaceutical Process,Shanghai 200437;2.Zhejiang Medicine Co.,Ltd.,Xinchang 312500) |
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| Abstract: | Solifenacin succinate was synthesized from phenethylamine by acylation,Bischler-Napieralski cyclization,reduction by NaBH4 and resolution to afford(S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline(6),which was subjected to condensation,ester exchange and then salification with an overall yield of about 21%. |
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| Keywords: | solifenacin overactive bladder synthesis |
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