| 引用本文: | 戴荣华,王栋,曾庆磊,郝双红.雷沙吉兰甲磺酸盐的合成工艺研究[J].中国现代应用药学,2016,33(1):56-58. |
| DAI Ronghua,WANG Dong,ZENG Qinglei,HAO Shuanghong.Synthetic Process of Rasagiline Mesylate[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(1):56-58. |
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| 摘要: |
| 目的 优化雷沙吉兰甲磺酸盐合成工艺。方法 1-茚酮经一锅法还原-胺化制得1-氨基茚满，然后与3-溴丙炔反应得N-炔丙基-1-氨基茚满，用L-酒石酸拆分得R-(+)-N-炔丙基-1-氨基茚满酒石酸盐，最后碱化、成盐得雷沙吉兰甲磺酸盐。结果 中间体及目标产物结构经1H-NMR和MS确证结构，5步总收率达19.2%。结论 此路线原料易得，反应条件温和，操作简便，收率高，适于工业化生产。 |
| 关键词: 雷沙吉兰甲磺酸盐 1-氨基茚满 合成 |
| DOI： |
| 分类号:R916.41 |
| 基金项目: |
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| Synthetic Process of Rasagiline Mesylate |
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DAI Ronghua1, WANG Dong2, ZENG Qinglei2, HAO Shuanghong2
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1.Jingbo Agrochemicals Technology Co. Ltd., Boxing 256500, China;2.Research Center of Agro-bionic Engineering & Tech. of Shandong Province, College of Chemistry & Pharm, Qingdao Agricultural University, Qingdao 266109, China
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| Abstract: |
| OBJECTIVE To optimize the synthetic process of rasagiline mesylate. METHODS First, 1-indanamine was synthesized from 1-indanone via reduction and amination. Then, R-(+)-N-propargyl-1-indanamine tartrate was obtained from 1-indanamine by condensation with 3-propargyl bromide, followed by resolution with L-tartaric acid. Finally, Rasagiline mesylate was prepared by alkalization and mesylation of the R-isomer L-tartrate. The total yield was 19.2%. RESULTS The chemical structures of intermediates and target product were confirmed by 1H-NMR and MS. CONCLUSION This synthetic process is characterized by cheap materials, mild condition, simple operation and high yield, and is fitting for industrial application. |
| Key words: rasagiline mesylate 1-indanamine synthesis |
