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Gabapentin preparation method

A gabapentin and drop-adding technology, which is applied in the field of gabapentin preparation, can solve the problems of low yield of gabapentin and achieve the effect of increasing yield and high yield

Inactive Publication Date: 2015-11-18
TAICANG YUNTONG BIOCHEM ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Adjunctive therapy for patients with focal seizures that cannot be satisfactorily controlled or tolerated by conventional antiepileptic drugs, and for patients with focal seizures followed by generalized seizures
[0003] The yield of gabapentin prepared in the prior art is low

Method used

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  • Gabapentin preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Put 1mol of cyclohexanone and 2mol of methyl cyanoacetate in a reaction kettle, add 3.0g of ammonium acetate and 10g of methanol as solvent, start stirring, cool to -5°C in an ice-salt bath, slowly add 3mol of ammonia water dropwise to continue the reaction Stir for 3 hours, remove the ice-salt bath, rise to room temperature and let stand for 20 hours, filter and dry to obtain α,α'-dicyano-1,1-cyclohexyldiacetimide ammonium salt; in high temperature liquid water at 160°C Add α,α'-dicyano-1,1-cyclohexyldiacetimide ammonium salt in batches to prevent a large number of bubbles from splashing out of the raw materials during the feeding process, heat to reflux, and obtain after crystallization, suction filtration, and drying Cyclohexyl diacetic acid; add 1.3 mol of urea to 1 mol of cyclohexyl diacetic acid, heat for 2 hours, add 50% ethanol-water solution after cooling to room temperature, heat to reflux, obtain 3,3- Pentamethylene glutarimide; Dissolve 0.12mol of 3,3-pentam...

Embodiment 2

[0022] Put 1mol of cyclohexanone and 3mol of methyl cyanoacetate in a reaction kettle, add 30g of ammonium acetate and 300g of methanol as solvent, start stirring, cool to -5°C in an ice-salt bath, slowly add 3mol of ammonia water dropwise and continue to stir 3h, remove the ice-salt bath, rise to room temperature and let it stand for 20h, filter and dry to prepare α,α'-dicyano-1,1-cyclohexyldiacetimide ammonium salt; dissolve in high temperature liquid water at 190°C Add α,α'-dicyano-1,1-cyclohexyldiacetimide ammonium salt in batches to prevent a large number of bubbles from splashing out the raw materials during the feeding process, heat to reflux, crystallize, suction filter, and dry to obtain cyclo Hexyl diacetic acid; add 1.5 mol of urea to 1 mol of cyclohexane diacetic acid, heat for 4 hours, add 50% ethanol-water solution after cooling to room temperature, heat to reflux, obtain 3,3-penta Methylene glutarimide; 0.12mol of 3,3-pentamethylene glutarimide was dissolved in ...

Embodiment 3

[0024] Put 1mol of cyclohexanone and 2mol of methyl cyanoacetate in a reaction kettle, add 40g of ammonium acetate and 400g of methanol as solvents, start stirring, cool to -8°C in an ice-salt bath, slowly add 3mol of ammonia water dropwise to react and continue stirring 3h, remove the ice-salt bath, rise to room temperature and let it stand for 20h, filter and dry to prepare α,α'-dicyano-1,1-cyclohexyldiacetimide ammonium salt; dissolve in high temperature liquid water at 200°C Add α,α'-dicyano-1,1-cyclohexyldiacetimide ammonium salt in batches to prevent a large number of bubbles from splashing out the raw materials during the feeding process, heat to reflux, crystallize, suction filter, and dry to obtain cyclo Hexyl diacetic acid; add 1.6 mol of urea to 1 mol of cyclohexane diacetic acid, heat for 4 hours, add 50% ethanol-water solution after cooling to room temperature, heat to reflux, obtain 3,3-penta Methylene glutarimide: Dissolve 0.2mol of 3,3-pentamethylene glutarimid...

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Abstract

The invention discloses a gabapentin preparation method. The gabapentin preparation method comprises the following steps: (1) placing cyclohexanone and methyl cyanoacetate into a reaction kettle, adding ammonium acetate and methanol, stirring, slowly adding ammonia water into a low-temperature bath for reaction, filtering and then preparing to obtain alpha,alpha'-dicyano-1,1-cyclohexanediacetylimide ammonium salt; (2) adding alpha,alpha'-dicyano-1,1-cyclohexanediacetylimide ammonium salt into high-temperature liquid water in batches to prepare cyclohexanediacetic acid; (3) adding urea into cyclohexanediacetic acid, heating up for reaction, then cooling, and adding the cooled product into an ethanol-water solution to prepare 3,3-pentamethylene glutarimide; (4) dissolving 3,3-pentamethylene glutarimide into a sodium hydroxide water solution, dripping a sodium hypochlorite and sodium hydroxide mixed solution for reaction, dripping hydrochloric acid to adjust the pH to prepare a gabapentin hydrochloride; (5) dissolving the gabapentin hydrochloride into sodium hydroxide to prepare gabapentin. The preparation method has the advantages that the raw materials are easy to obtain, and the yield of the prepared product is high.

Description

technical field [0001] The invention relates to the technical field of gabapentin, in particular to a preparation method of gabapentin. Background technique [0002] Gabapentin, whose scientific name is 1-(aminomethyl)cyclohexaneacetic acid, is a novel antiepileptic drug, which is a derivative of γ-aminobutyric acid (GABA), and its pharmacological effects are different from those of existing antiepileptic drugs. Recent studies have shown that the effect of gabapentin is to alter the metabolism of GABA. Gabapentin has been shown to prevent epilepsy in various animal models. In addition, it has also shown effects in animal models of spasticity, analgesia and amyotrophic lateral sclerosis. Gabapentin has a high affinity for novel binding sites in brain tissue, and it can pass through some barriers in the body through amino acid transfer bodies. Compared with other anticonvulsant drugs, gabapentin has less behavioral and cardiovascular side effects. Gabapentin has a high affin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/28C07C227/12C07C227/04
Inventor 张卫东
Owner TAICANG YUNTONG BIOCHEM ENG
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