PREPARATION OF ASEPTIC 3-2-4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYLETHYL-6,7,8,9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDIO1,2-APYRIMIDIN-4-ONE PALMITATE ESTER

摘要

The present invention concerns a process for preparing aseptic crystalline 3-[2-[4- (6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy- 2-methyl-4H-pyrido[l,2-a]pyrimidin-4-one palmitate ester (I) substantially free of 3-[2-[4-(6-fluoro- 1 ,2-benzisoxazol-3-yl)- 1 -piperidinyl]ethyl]-6,7,8,9-tetrahydro-9- hydroxy-2-methyl-4H-pyrido[ 1 ,2-a] pyrimidin-4-one (II-a), 3-[2-[4-(6-fluoro-l ,2- benzisoxazol-3-yl)-l-piperidinyl]ethyl]-6,7-dihydro-2-methyl-4H-pyrido[l ,2-a]- pyrimidin-4-one (II-b), and 3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]- ethyl]-6,7,8,9-tetrahydro-2-methyl-9-pentadecyl-4H-pyrido[l ,2-a]pyrimidin-4-one (III), and having an average particle size ranging from 20 to 150 μm.