abstract |
The present invention provided a process for the preparation of gabapentin hydrochloride. The process comprises: conventing 1,5-dicyano-2,4-dioxo-3-azaspiro[5,5]undecane into 1,5-dicarbamoyl-2,4-dioxo-3-azaspiro[5,5]undecane at a temperature between 65 to 85 and in the presence of strong acid, then carrying out the Hoffmann rearrangement reaction in the presence of base. The starting material of present process is readily available. The process is simple, and can decrease the purification procedure for the intermediate, reduce the cost, and obtain the product with high purity. |