Method for lipase-catalyzed online synthesis of N-(5-vinyl ester valeryl)mexiletine

A technology for vinyl ester valeryl and mexiletine, which is applied in the field of lipase catalyzed on-line controllable and selective synthesis of N-mexiletine, can solve the problems of low bioavailability, short half-life, long reaction time and the like, and shorten the reaction time. Time, high conversion and selectivity, effect of reducing reaction cost
CN107488683AInactive Publication Date: 2017-12-19ZHEJIANG UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG UNIV OF TECH
Publication Date
2017-12-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for lipase-catalyzed online synthesis of N-(5-vinyl ester valeryl)mexiletine. The method, adopting mexiletine and divinyl adipate with a molar ratio of 1:(1-6) as raw materials, dimethyl sulphoxide and tertiary amyl alcohol with a volume ratio of 1:(1-10) as a reaction solvent and lipase Lipozyme TL IM as a catalyst, comprises the following steps: placing the raw materials and the reaction solvent in a syringe, uniformly filling the reaction channel of a micro-fluidic channel reactor with the lipase Lipozyme TL IM, and continuously introducing the raw materials and the reaction solvent into the reaction channel reactor under the push of a syringe pump, wherein the internal diameter of the reaction channel of the micro-fluidic channel reactor is 0.8-2.4 mm, and the length of the reaction channel is 0.5-1.0 m; and carrying out an acylation reaction at a temperature of 30-70 DEG C for 20-40 min, online collecting the obtained reaction solution through a product collector, and routinely post-processing the reaction to obtain the N-(5-vinyl ester valeryl)mexiletine. The method has the advantages of short reaction time, high selectivity and high yield.
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Description

(1) Technical field

[0001] The invention relates to a method for synthesizing N-(5-vinylvaleryl) mexiletine on-line with controllable selectivity catalyzed by lipase. (2) Background technology

[0002] Currently, small-molecule drugs are the mainstream of clinically used drugs. However, small-molecule drugs have fast metabolism, short half-life and obvious peak-valley effect, which lead to frequent administration. Small-molecule drugs are prepared by chemical biology methods to prepare new drug derivatives. Or sugar-containing drug derivatives and polymer prodrugs of drugs are an effective method to improve drug sustained release and targeting.

[0003] At this stage, most drugs are facing the problem of too high fat solubility or poor water solubility, and the existence of these problems leads to poor gastrointestinal absorption of drugs and poor oral bioavailability. To this end, researchers have increased the water solubility and oral bioavailability of drugs through wat...

Claims

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