甲磺酸沙芬酰胺合成工艺改进

黄 建1,毕光庆1,谢建树1,吴嘉杰2

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主办:上海医药工业研究院
   中国药学会
   中国化学制药工业协会
ISSN 1001-8255   CN 31-1243/R   ZYGZEA
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中国医药工业杂志 ›› 2016, Vol. 47 ›› Issue (07) : 828. DOI: 10.16522/j.cnki.cjph.2016.07.001
化学药物与合成技术 Chemical Drug & Synthetic Technology

甲磺酸沙芬酰胺合成工艺改进

作者信息 +

Improved Synthesis of Safinamide Mesilate

Author information +
History +

摘要

3- 氟苄氯与对羟基苯甲醛在有机碱作用下缩合制得4-( 3- 氟苄氧基) 苯甲醛,然后与L- 丙氨酰胺盐酸盐经亚胺生成、还原及成盐一锅反应制得帕金森病治疗药物甲磺酸沙芬酰胺,总收率约79.6%。该法反应条件温和,选择性高,适合工业化生产。

Abstract

An improved synthetic process of safinamide mesilate with an overall yield of 79.6% was described, which comprised the condensation of 3-fluorobenzyl chloride with 4-hydroxybenzaldehyde in the presence of organicbase, followed by reaction with L-alaninamide hydrochloride via a one-pot imine generation, reduction and salification.The process had the advantages of mild reaction condition and high reaction selectivity with good potential for industrial application.

关键词

甲磺酸沙芬酰胺 / 帕金森病 / 工艺改进

Key words

safinamide mesilate / parkinson's disease / improved synthesis

引用本文

导出引用
黄 建1,毕光庆1,谢建树1,吴嘉杰2. 甲磺酸沙芬酰胺合成工艺改进. 中国医药工业杂志. 2016, 47(07): 828 https://doi.org/10.16522/j.cnki.cjph.2016.07.001
HUANG Jian1, BI Guangqing1, XIE Jianshu1, WU Jiajie2. Improved Synthesis of Safinamide Mesilate. Chinese Journal of Pharmaceuticals. 2016, 47(07): 828 https://doi.org/10.16522/j.cnki.cjph.2016.07.001

参考文献

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[2] 陈其龙, 徐美华, 董文心. 帕金森病治疗药物的临床应用进展[J]. 世界临床药物, 2011, 32(6): 324—328.

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