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局部麻醉药盐酸达克罗宁高效合成工艺

卢定强 严国荣 王新仙 吉文哲 刘桐岐 凌岫泉

生物加工过程2016,Vol.14Issue(5):65-69,5.
生物加工过程2016,Vol.14Issue(5):65-69,5.DOI:10.3969/j.issn.1672-3678.2016.05.012

局部麻醉药盐酸达克罗宁高效合成工艺

Synthesis of local anesthetic dyclonine hydrochloride

卢定强 1严国荣 2王新仙 1吉文哲 1刘桐岐 1凌岫泉1

作者信息

  • 1. 南京工业大学 药学院,江苏 南京 211800
  • 2. 江苏省药物研究所,江苏 南京 210009
  • 折叠

摘要

Abstract

Dyclonine hydrochloride is commonly used as local anesthetics. We developed an efficient synthesis process of dyclonine hydrochloride, namely a novel two-step synthesis process. In this process, 4-hydroxyacetophenone and n-butyl bromide were used as the starting material, the intermediate 1-( 4-butoxyphenyl )-ethanone was produced by using the phase-transfer catalyst, and then dyclonine hydrochloride was obtained by further reacting with piperidinium chloride and paraformaldehyde. The structures of dyclonine hydrochloride were confirmed by 1 H-NMR and MS. The overall yield was more than 90%. It is an easy operation process and suitable for industrial production.

关键词

盐酸达克罗宁/相转移催化剂/合成工艺

Key words

dyclonine hydrochloride/phase-transfer catalyst/synthesis process

分类

医药卫生

引用本文复制引用

卢定强,严国荣,王新仙,吉文哲,刘桐岐,凌岫泉..局部麻醉药盐酸达克罗宁高效合成工艺[J].生物加工过程,2016,14(5):65-69,5.

基金项目

国家自然科学基金 ()

生物加工过程

OACSTPCD

1672-3678

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