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A kind of method of synthesizing mexiletine hydrochloride

A technology for mexiletine and hydrochloride, which is applied in the field of synthesizing mexiletine hydrochloride, can solve the problems of high toxicity, high price, and large amount of chlorinated acetone, and achieves no environmental hazard, high economy, and reaction yield. high effect

Active Publication Date: 2021-11-09
NANJING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The limitation of this method is that the raw material chloroacetone is very toxic and expensive, and NaBH 3 CN is also a highly toxic compound and is used in large quantities

Method used

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  • A kind of method of synthesizing mexiletine hydrochloride
  • A kind of method of synthesizing mexiletine hydrochloride
  • A kind of method of synthesizing mexiletine hydrochloride

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Embodiment Construction

[0030] The following examples are presented to illustrate certain embodiments of the invention and should not be construed as limiting the scope of the invention. Many modifications, variations and changes can be made to the disclosed content of the present invention simultaneously in terms of materials, methods and reaction conditions. All such modifications, changes and alterations are surely within the spirit and scope of the invention.

[0031] Embodiment: mexiletine hydrochloride

[0032] N-chloro-1-(2,6-dimethylphenoxy)propan-2-amine

[0033]

[0034] 2,6-Dimethylphenol (1.2g, 10mmol), potassium carbonate (2.8g, 20mmol) and acetone (20ml) were added into a round bottom flask and stirred for 10min, then 3-bromopropyne (1.8mg, 15 mmol), and stirred at room temperature for at least 6 hours to obtain a yellow mixture which was collected by filtration. The resulting intermediate (160mg, 1.0mmol), cat.[Au] (6mg, 1mmol%), AgOTf (2.6mg, 1mmol%), water (36mg, 2mmol) and met...

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Abstract

The invention discloses a method for synthesizing mexiletine hydrochloride. In the reaction system, 2,6-dimethylphenol is used as the initial raw material to synthesize the corresponding target product. In the reaction, a transition metal gold complex and a rhodium complex are used. Compared with the previous method for synthesizing mexiletine hydrochloride, the present invention does not add any alkali in the reaction process, produces no by-products, has high reaction atom economy and mild reaction conditions. Therefore this invention has broad development prospect.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis chemistry, and in particular relates to a method for synthesizing mexiletine hydrochloride. Background technique [0002] Mexiletine hydrochloride is a class of important compounds widely used in the field of medicine. It is a calcium channel blocker and belongs to class Ib antiarrhythmic drugs. It is mainly used for the treatment of acute and chronic ventricular arrhythmias. This type of compound is synthesized by the following method, 2,6-dimethylphenol reacts with chloroacetone, and then, in NaBH 3 Synthesis by reductive amination reaction with the participation of CN (European Journal of Medicinal Chemistry, 121, 300-307; 2016) [0003] [0004] The limitation of this method is that the raw material chloroacetone is very toxic and expensive, and NaBH 3 CN is also a highly toxic compound and is used in large quantities. Therefore, from the perspective of organic synthesis, it is...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C217/54C07C213/06C07C213/08C07C41/16C07C43/215C07C45/26C07C49/175
CPCC07C41/16C07C45/26C07C213/06C07C213/08C07C43/215C07C49/175C07C217/54
Inventor 李峰李顺徐梦
Owner NANJING UNIV OF SCI & TECH