Synthesis process of gabapentin intermediate

Abstract

The invention relates to a synthesis process of a gabapentin intermediate. The intermediate is 1, 1-cyclohexyldiacetic acid. the synthesis process comprises the following steps: cyclizing cyclohexanone and ethyl cyanoacetate to prepare alpha, alpha'-dicyano-1, 1-cyclohexyldiacetylimine ammonium salt, and then hydrolyzing under the action of solid acid to prepare a target product intermediate. The solid acid is prepared by taking montmorillonite intercalated with modified cellulose as a carrier, loading tin ions through an ion exchange method and then carbonizing at low temperature. The synthesis of the gabapentin intermediate is realized by utilizing the self-made solid acid catalyst, the green and environment-friendly concept is compounded, and meanwhile, the yield is relatively high; each preparation process of the catalyst is relatively simple, complicated post-treatment is not needed, the catalyst can be recycled, and the repeated utilization rate is high; and the corrosion of concentrated sulfuric acid to industrial equipment and the pollution to the environment in the traditional process are avoided, and the treatment cost of waste liquid in the later period is reduced.

Description

technical field [0001] The invention relates to the technical field of chemical synthesis, in particular to a synthesis process of a gabapentin intermediate. Background technique [0002] Gabapentin, chemically known as aminomethylcyclohexylacetic acid, is a new type of antiepileptic drug. At present, there are more and more mature synthetic routes for the synthesis of gabapentin, and the yield and purity of the product have been improved. A relatively mature synthetic method, such as using cyclohexanone as a raw material, undergoes multi-step reactions, including cyclization, hydrolysis, condensation and Hofmann degradation, to obtain the target product gabapentin. 1,1-cyclohexyl diacetic acid It is an important intermediate in the reaction process. The existing process is to use gap kettle reaction, except that the reaction itself consumes a large amount of concentrated sulfuric acid, which seriously pollutes the environment; high concentration of concentrated sulfuric ...

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Problems solved by technology

1,1-cyclohexyl diacetic acid It is an important intermediate in the reaction process. The existing process uses gap kettle reaction. In addition to the large consumption of concentrated sulfuric acid in the reaction itself, it seriously pollutes the environment; high concentration of concentrated sulfuric acid will also corrode equipment and seriously affect product quality.

[0003] Compared with liquid acid catalysts, solid acid catalysts have the characteristics of stable properties, easy reuse, and less environmental pollution. Carbon-based solid acid catalysts prepared from carbohydrates have been widely studied and applied. However, gabapentin However, there are few reports on the use of solid acid in the synthesis process

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