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Title:
METHOD FOR PREPARING LIDOCAINE INTERMEDIATE α-CHLOROACETYL-2,6-DIMETHYLANILINE AND LIDOCAINE WITHOUT ADDING ADDITIONAL ALKALI
Document Type and Number:
WIPO Patent Application WO/2021/159754
Kind Code:
A1
Abstract:
The present invention relates to a method for preparing an lidocaine intermediate α-chloroacetyl-2,6-dimethylaniline and lidocaine without adding additional alkali, belonging to the technical field of organic synthesis. A method for preparing the lidocaine intermediate α-chloroacetyl-2,6-dimethylaniline without adding additional alkali is as follows: in the process of generating α-chloroacetyl-2,6-dimethylaniline by performing a chloroacetylation reaction of 2,6-dimethylaniline and chloroacetyl chloride, taking a mixed solution of one or more of an alkane solvent, an ether solvent and an ester solvent as an organic solvent. As a separation process can be reduced by not adding additional alkali, the method can be applied to a one-pot reaction so as to directly prepare lidocaine, i.e. 2,6-dimethylaniline and chloroacetyl chloride directly reacts with diethylamine so as to obtain lidocaine. The method is simple without adding additional alkali, and the separation process is simplified. The used solvent is a third-type solvent. The method is safer in operation, and the obtained product is high in purity, high in yield, low in cost and environmentally friendly.

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Inventors:
WU XIAOJUN (CN)
WANG YOUQING (CN)
FENG YUNXIA (CN)
JIANG DEGANG (CN)
ZHANG GAOFENG (CN)
SHEN LIKUN (CN)
YANG YONG (CN)
XIAO CHUHUI (CN)
Application Number:
PCT/CN2020/125134
Publication Date:
August 19, 2021
Filing Date:
October 30, 2020
Export Citation:
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Assignee:
ZHENGZHOU YUANLI BIOLOGICAL TECH CO LTD (CN)
International Classes:
C07C231/02; C07C231/12; C07C231/24; C07C233/07
Foreign References:
US20120022147A12012-01-26
CN110117233A2019-08-13
CN102070483A2011-05-25
CN110642738A2020-01-03
Attorney, Agent or Firm:
ZHENGZHOU RUIXIN INTELLECTUAL PROPERTY AGENCY CO., LTD. (CN)
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