4-二甲胺基丁醛二乙基缩醛的合成

J4 ›› 2011, Vol. 24 ›› Issue (5): 1-4.

4-二甲胺基丁醛二乙基缩醛的合成

冯润良¹, 陈修毅², 宋智梅^1*, 岳冬玲³

1．济南大学医学与生命科学学院，山东济南 250022； 2.山东省医药工业研究所，山东济南 250101； 3.辽宁海思科制药有限公司，辽宁兴城 125107

收稿日期:2011-04-30 出版日期:2011-10-20 发布日期:2011-10-20
作者简介:冯润良（1970-），男，博士，副教授，主要从事药学教学及科研。
基金资助:
济南大学科研基金（XKY1010）；济南大学教研项目（JQ0913）

4-Dimethylaminobutyraldehyde diethyl acetal

FENG Run-Liang¹, CHEN Xiu-Yi², SONG Zhi-Mei^1*, YUE Dong-Ling³

1.School of Medical and Life Sciences, University of Jinan, Jinan 250022, China; 2.Shandong Institute of Pharmaceutical Industry, Jinan 250101, China; 3.Haisike Pharmaceuticals Co. Ltd., Xingcheng 125107, China

Received:2011-04-30 Online:2011-10-20 Published:2011-10-20

摘要/Abstract

摘要：

4-二甲胺基丁醛二乙基缩醛是制备治疗偏头痛的曲坦类药物的关键中间体，其合成工艺的优劣对药物的合成成本有重要影响。本文以1-溴-3-氯丙烷为起始原料，与二甲胺水溶液经相转移催化剂聚乙二醇催化得到3-二甲胺基-1-氯丙烷，然后于2-甲基四氢呋喃中与镁反应制得格氏试剂，而后与原甲酸三乙酯反应得到目标化合物。该路线总收率70.11%，路线简单、污染低、易操作、收率高。

关键词: 4-二甲胺基丁醛二乙基缩醛, 合成, 舒马曲坦

Abstract:

4-Dimethylaminobutyraldehyde diethyl acetal is a key intermediate for the preparation of anti-migraine drugs. Its synthesis technique significantly affects the production cost of anti-migraine drugs. We catalyzed the reaction of 1-bromo-3-chloro propane and dimethylamine solution with PEG as a phase transfer catalyst, and obtained 3-dimethylamino-1-chloro propane. 3-dimethylamino-1-chloro propane reacted with magnesium and Grinard reagent was acquired. We eventually obtained our target compound by the reaction of Grinard reagent and triethyl orthoformate. The total recovery rate of our target compound was 70.11%. The advantages of this method are simple operation, low environment pollution, high recovery rate and easy implementation.

Key words: 4-dimethylaminobutyraldehyde diethyl acetal, synthesis, Sumartriptan

中图分类号:

冯润良, 陈修毅, 宋智梅, 岳冬玲. 4-二甲胺基丁醛二乙基缩醛的合成[J]. J4, 2011, 24(5): 1-4.

FENG Run-Liang, CHEN Xiu-Yi, SONG Zhi-Mei, YUE Dong-Ling. 4-Dimethylaminobutyraldehyde diethyl acetal[J]. J4, 2011, 24(5): 1-4.

参考文献

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