| 镇痛药盐酸曲马多的合成工艺改进 |
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| 引用本文： | 钟为慧,吴窈窕,张兴贤,苏为科.镇痛药盐酸曲马多的合成工艺改进[J].中国药物化学杂志,2008,18(6):426-428. |
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| 作者姓名： | 钟为慧 吴窈窕 张兴贤 苏为科 |
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| 作者单位： | 浙江工业大学,制药工程教育部重点实验室,浙江,杭州,310014 |
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| 摘 要： | 目的研究镇痛药盐酸曲马多的合成工艺。方法以环己酮为起始原料,用绿色溶剂2-甲基四氢呋喃（2-MeTHF）替代四氢呋喃,经Mannich反应、格氏反应、通氯化氢成盐等反应得到目标化合物盐酸曲马多。结果与结论目标化合物的结构经1H-NMR、MS谱确证。总收率为76.7%,（E）-盐酸曲马多异构体含量99.44%。改进后的工艺,操作简单,综合成本低,环境污染小,更适合工业化生产。
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| 关 键 词： | 盐酸曲马多 镇痛药 2-甲基四氢呋喃 合成 |
| 收稿时间： | 2008-4-16 |
| 修稿时间： | 2008-9-20 |
Improved synthesis of tramadol hydrochloride |
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| ZHONG Wei-hui,WU Yao-tiao,ZHANG Xing-xian,SU Wei-ke.Improved synthesis of tramadol hydrochloride[J].Chinese Journal of Medicinal Chemistry,2008,18(6):426-428. |
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| Authors: | ZHONG Wei-hui WU Yao-tiao ZHANG Xing-xian SU Wei-ke |
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| Institution: | （Key Laboratory of Pharmaceutical Engineering of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, China） |
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| Abstract: | Aim To improve the synthetic procedure of tramadol hydrochloride.Methods Tramadol hydrochloride was synthesized starting from cyclohexanone via Mannich reaction,Grignard reaction and hydrochloride precipitation.In this case,2-methyltetrahydrofuran(2-MeTHF) was used instead of THF in the formation and reaction of Grignard reagents.Results and conclusion The structure of target compound was confirmed by 1H-NMR,MS,and the overall yield was 76.7% with the purity of(E)-tramadol hydrochloride 99.44%(HPLC).By the advantage of improved environmental friendly process with convenient operation,higher yield,lower cost,it is suitable for large scale manufacture. |
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| Keywords: | tramadol hydrochloride analgesics 2-methyltetrahydrofuran synthesis |
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