181289-23-6Relevant articles and documents
METHOD FOR PREPARING PREGABALIN
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Paragraph 0044; 0047; 0050; 0053; 0056, (2021/04/23)
The present invention relates to a method for preparing pregabalin by a biological enzyme method. In particular, the method comprises producing pregabalin B and an R-configuration compound C by using a compound A as a raw material under the action of a biological enzyme; performing configuration inversion of the separated and recovered R-configuration compound C under the action of an isomerase to produce an S-configuration compound D; and producing pregabalin B from the compound D under the action of a biological enzyme
Method for synthesizing and refining (S)- pregabalin (by machine translation)
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Paragraph 0041-0044; 0050-0053; 0059-0062, (2020/04/17)
The reaction conditions of the method disclosed by the invention are mild, and the method disclosed by the invention is mild in reaction conditions: (S)- kg of crude,methylhexanoic acid is obtained through: degradation, the reaction conditions of the intermediate (R)- (-) - 3 - (isobutyl - 2 2-pyrrolidinone) - 5 - are more moderate, and the reaction conditions of the preparation method, Hoffman are obtained (S)- times by weight, of the preparation method for, pregabalin concentrate (S)- 4 - obtained by hydrolysis-ring; of the raw material, to obtain a high-purity pregabalin intermediate solution (S)- obtained by carrying out hydrolysis (S)- on a crude product with a high purity,methyl.methylhexanoic acid after re-crystallization, to, obtain a high,purity pregabalin product. (by machine translation)
Synthetic method of environment-friendly and efficient pregabalin
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, (2019/02/04)
The invention relates to a synthetic method of environment-friendly and efficient pregabalin. The synthetic method comprises the following steps: 1) dehydrating and condensing acetate and isopentyl aldehyde to obtain 5-methyl-2-hexenoate; 2) performing cyano addition on the 5-methyl-2-hexenoate to obtain (S)-5-methyl-3-cyanohexanoate; 3) performing hydrogen reduction cyclization on the (S)-5-methyl-3-cyanohexanoate to obtain (S)-4-isobutylpyrrolidin-2-one; and 4) performing hydrolysis and ring opening on the (S)-4-isobutylpyrrolidin-2-one to obtain the pregabalin. The synthetic route has the advantages of cheap and easily available raw materials, few reaction steps, mild process conditions, simple operation, high reaction yield and less environment pollution, and is more suitable for industrial production of bulk drug pregabalin.