PROCESS FOR THE PREPARATION OF RISPERIDONE

摘要

The invention provides a more handy and environment friendly process for preparing risperidone, which comprises reacting 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride with 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2a] pyrimidin-4-one in a basic aqueous solution. The concentration of alkali metal carbonate in the basic aqueous solution is ranged from 15% to 40%. The reaction is carried out at temperature range of 101-140°C and the reaction is completed within 10 minutes to 2 hours.