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Improved process for production of gabapentin intermediate

A reaction and product technology, applied in the field of improvement for the preparation of gabapentin intermediates, can solve the problems of impractical gaseous NH3 and low efficiency of Guareschi reaction

Inactive Publication Date: 2004-01-28
TEVA PHARMA IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0007] The Guareschi reaction is inefficient as it takes at least 48 hours to complete, more usually between 48-168 hours
In addition, current environmental regulations allow the large-scale production of gaseous NH dissolved in ethanol 3 unrealistic

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0016] Into a three-neck round bottom flask equipped with a reflux condenser, thermometer and stirrer was charged 264.4 grams of ethyl cyanoacetate and 312 grams of methanol. The solution was cooled to 8°C while stirring. 2 g of ammonium acetate and 1 equivalent of cyclohexanone were added at 8°C. 60 g of a 25% strength ammonium hydroxide solution are added within 1 hour. During the addition of ammonium hydroxide, the temperature of the reaction mixture was maintained at 8-11°C. The solution was kept at 8-11°C for another half hour. Cooling was stopped and the temperature of the reaction mixture was allowed to rise to 25°C over 45 minutes. The suspension was kept at 25°C for 20 hours. After 20 hours, the suspension was slightly heated and 50% sulfuric acid was added until pH 2. During acidification, the temperature was maintained at 50-55°C. The reaction was cooled to 12°C, the suspension was stirred at 12°C for half an hour and then filtered. The filter cake was washed...

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Abstract

The invention relates to a novel process for producing a the intermediary compound alpha , alpha ', dicyano- beta , beta - pentamethyleneglutarimide. The process includes the steps of reacting a ketone such as cyclohexanone with ethylcyanoacetate in the presence of ammonium hydroxide.

Description

[0001] Cross References to Related Applications [0002] This application claims priority under 35 U.S.C. 119(e) to U.S. Provisional Application No. 60 / 244891, filed November 2, 2001, which is incorporated herein by reference. technical field [0003] The present invention relates to a compound used as an intermediate in the preparation of gabapentin, and a preparation method thereof. More specifically, the present invention relates to α,α'-dicyano-β,β-pentylidene glutarimide, and the preparation of α,α'-dicyano-β,β-pentyleneglutaryl imine method. Background technique [0004] Gabapentin, 1-(aminomethyl)-1-cyclohexaneacetic acid, has the chemical structure of Formula I: [0005] Gabapentin is used to treat brain disorders such as epilepsy, fainting seizures, hypokinesia, and cranial trauma. U.S. Patent 4,024,175 to Satzinger et al., which is incorporated herein by reference, discloses that gabapentin of formula (I) exhibits warming properties and, in some cases, anesthe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/00C07D221/20
CPCC07D221/20C07D211/88
Inventor S·M·P·蒙塔纳里
Owner TEVA PHARMA IND LTD
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