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

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4-Dimethylaminobutyraldehyde diethyl acetal

 FENG Run-Liang1, CHEN Xiu-Yi2, SONG Zhi-Mei1*, YUE Dong-Ling3   

  1. 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 Published:2011-10-20 Online:2011-10-20

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

CLC Number: 

  • O62

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