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Preparation method of gabapentin

A technology for gabapentin and gabapentin hydrochloride, which is applied in the field of gabapentin preparation, can solve the problems of long lines and cumbersome post-processing, and achieve the effects of simple preparation process, simplified post-processing process, and easy availability of raw materials

Inactive Publication Date: 2014-12-24
TAICANG YUNTONG BIOCHEM ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing gabapentin preparation method has long lines, cumbersome post-treatment, and produces a large amount of acidic waste liquid

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1: the preparation method of a kind of gabapentin of the present embodiment, comprises the following steps:

[0017] (1) 1,1-cyclohexyl diacetic acid was placed in the reactor, heated to 80 ° C, after being pressurized to 6Mpa, passed carbon dioxide and ammonia gas to react for 0.5 hour, first cooled the reaction solution, added isopropanol solution After that, heating to reflux, filtration, recrystallization and drying to obtain 3,3-pentamethylene glutaramide;

[0018] (2) Dissolve 3,3-pentamethylene glutaramide in a sodium bicarbonate solution with a concentration of 30%, leave it for 10 hours, first add a 15% hydrogen peroxide solution, then add hydrochloric acid to neutralize the pH to below 1, to obtain gabapentin hydrochloride;

[0019] (3) adding gabapentin hydrochloride into a 30% sodium hydroxide solution and heating to 60° C. to dissolve, adding activated carbon to absorb impurities, then filtering, evaporating to dryness under reduced pressure, re...

Embodiment 2

[0020] Embodiment 2: the preparation method of a kind of gabapentin of the present embodiment, comprises the following steps:

[0021] (1) 1,1-cyclohexyl diacetic acid was placed in the reactor, heated to 110 ° C, after being pressurized to 8Mpa, passed carbon dioxide and ammonia gas to react for 1.5 hours, cooled the reaction solution first, and added isopropanol solution After that, heating to reflux, filtration, recrystallization and drying to obtain 3,3-pentamethylene glutaramide;

[0022] (2) Dissolve 3,3-pentamethylene glutaramide in a sodium bicarbonate solution with a concentration of 30%, leave it for 10 hours, first add a 15% hydrogen peroxide solution, then add hydrochloric acid to neutralize the pH to below 1, to obtain gabapentin hydrochloride;

[0023] (3) adding gabapentin hydrochloride to a concentration of 30% sodium hydroxide solution and heating to 80° C. to dissolve, adding activated carbon to absorb impurities, then filtering, evaporating to dryness under...

Embodiment 3

[0024] Embodiment 3: the preparation method of a kind of gabapentin of the present embodiment, comprises the following steps:

[0025] (1) 1,1-cyclohexyldiacetic acid is placed in the reactor, heated to 90 ° C, after being pressurized to 7Mpa, feed carbon dioxide and ammonia gas to react for 1 hour, cool the reaction solution first, add isopropanol solution After that, heating to reflux, filtration, recrystallization and drying to obtain 3,3-pentamethylene glutaramide;

[0026] (2) Dissolve 3,3-pentamethylene glutaramide in a sodium bicarbonate solution with a concentration of 30%, leave it for 10 hours, first add a 15% hydrogen peroxide solution, then add hydrochloric acid to neutralize the pH to below 1, to obtain gabapentin hydrochloride;

[0027] (3) adding gabapentin hydrochloride into a 30% sodium hydroxide solution and heating to 70° C. to dissolve, adding activated carbon to absorb impurities, then filtering, evaporating to dryness under reduced pressure, recrystalliz...

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PUM

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Abstract

The invention discloses a preparation method of gabapentin. The preparation method comprises the following steps: (1) placing 1,1-cyclohexyl diacetic acid into a reaction kettle, heating and pressurizing, introducing carbon dioxide and ammonia gas, reacting for 0.5-1.5 hours, and purifying reaction liquid to obtain 3,3-pentamethyleneglutarimide; (2) dissolving 3,3-pentamethyleneglutarimide into sodium bicarbonate solution, firstly adding hydrogen peroxide solution, and then adding hydrochloric acid for neutralizing until pH is 1 below, to obtain gabapentin hydrochloride; and (3) adding gabapentin hydrochloride into sodium hydroxide solution and heating for dissolving, adding activated carbon to adsorb impurities, and then performing filtering, pressure-reduced evaporation, recrystallization and drying to obtain high-purity gabapentin. The preparation method is easy for obtaining of raw materials, low in cost, simple in preparation process, and less in generated waste liquid.

Description

technical field [0001] The invention relates to the technical field of antiepileptic chemical drugs, in particular to a preparation method of gabapentin. Background technique [0002] Gabapentin, also known as 1-(aminomethyl)cyclohexaneacetic acid, also known as 1-(methylamino)cyclohexaneacetic acid, the molecular formula is C 9 H 17 NO 2 , is a novel antiepileptic drug. Gabapentin has been shown to prevent epilepsy in various animal models, in addition, in animal models of spasticity, analgesia, and amyotrophic lateral sclerosis. Gabapentin has a high affinity for novel binding sites in brain tissue, it can pass through some barriers in the body through amino acid transfer bodies, and compared with other anticonvulsants, gabapentin has less behavioral and cardiovascular side effects. Gabapentin has a high affinity for novel binding sites in brain tissue, it can pass through some barriers in the body through amino acid transfer bodies, and compared with other anticonvuls...

Claims

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Application Information

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IPC IPC(8): C07C229/28C07C227/04C07C227/22
Inventor 张卫东
Owner TAICANG YUNTONG BIOCHEM ENG