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Citation: LI Yanqin, YU Fengli, ZHUANG Shengli. Improved Synthetic Method and Characterization of Emedastine Difumarate[J]. Chinese Journal of Applied Chemistry, ;2013, 30(11): 1285-1288. doi: 10.3724/SP.J.1095.2013.20601 shu

Improved Synthetic Method and Characterization of Emedastine Difumarate

a. Hangzhou Minsheng Pharmaceutical Group Co., Ltd., Hangzhou 310011, China;
b. College of Chemistry and Molecular Engineering, Qingdao University ofScience and Technology, Qingdao 266042, China

Received Date: 24 December 2012
Revised Date: 12 March 2013

Emedastine difumarate(1) was prepared via improved synthetic processes.After adding phase transfer catalyst,the synthesis of the two key intermediates such as 2-chloro-1-(2-ethoxyethyl) benzimidazole(4) and emedastine(5) for the reactions could be optimized.No water was needed for the reactions and the yields were significantly enhanced.Typically,the yields of compounds 4 and 5 are up to 67.9% and 74.9%,respectively.The structure of the prepared product was confirmed by IR,¹H NMR,¹³C NMR,MS,elemental analysis,differential thermal analysis,and X-ray powder diffraction.
- Emedastine difumarate,
- synthesis,
- characterization,
- phase transfer catalysts
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