Hao Xiaoyan
2010
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Journal
China Medical Herald
Abstract
Objective:To optimize synthetic process of a pyrimidine intermediate for risperidone,and to increase the yield.Methods:3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a] pyrimidin-4-one,the pyrimidine intermediate for the synthesis of the atypical antipsychotic agent risperidone,was synthesized from 2-aminopyridine and α-acetyl-γ-butyrolactone by cyclization and catalytic hydrogenation.Results:The synthetic process was improved,opera-tion was simplified and the overall yield was increased to 68.2%.The structure of the 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a] pyrimidin-4-one was identified by MS and 1H-NMR.Conclusion:The improved synthetic process is practicable and suitable for large-scale manufacture.