84163-46-2Relevant articles and documents
Purification method of 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride
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, (2021/04/10)
The invention discloses a purification method of a risperidone intermediate 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride as shown in a formula II, which is characterized by comprising the following steps: adding 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride into ethanol, adding a certain amount of water, and carrying out heating reflux until the solution is clear to obtain the risperidone intermediate 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride; and cooling the compound to a certain temperature for crystal growing, then cooling the mixture to -5 to 10 DEG C, and filtering and drying the mixture to obtain the crystal. According to the purification method of the 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride, the dimer shown as the formula V can be effectively separated out, the purification yield is 85% or above, the chemical purity of a finished product can reach 99.9% or above, an amplification effect cannot be generated in large-scale production, and the process is stable.
Process for making risperidone and intermediates therefor
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Page/Page column 5, (2008/06/13)
The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7). The oxime(s) can be isomerically enriched by a variety of techniques including the use of the novel acetic acid salt thereof, which affords, inter alia, resolution of the isomers and/or by heat conversion.