PREPARATION OF ASEPTIC 3-[2-[4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL]ETHYL]-6,7,8,9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDIO[1,2-A]PYRIMIDIN-4-ONE PALMITATE ESTER

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 -pi...

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Hauptverfasser: VERBRAEKEN, JURGEN, ALOIS, SPITTAELS, THOMAS, FREDERIK, ERNESTINE, VAN DUN, JOANNES, PETRUS, WOUTERS, BENNY
Format: Patent
Sprache:eng ; fre
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Zusammenfassung: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. L'invention concerne un procédé de préparation d'ester de 3-[2-[4- (6-fluoro-l,2-benzisoxazol-3-yl)-l-pipéridinyl]éthyl]-6,7,8,9-tétrahydro-9-hydroxy-2-méthyl-4H-pyrido[l,2-a]pyrimidin-4-one de palmitate cristallin aseptique (I) sensiblement exempt de 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-pipéridinyl]éthyl]-6,7,8,9-tétrahydro-9- hydroxy-2-méthyl-4H-pyrido[1,2-a] pyrimidin-4-one (II-a), 3-[2-[4-(6-fluoro-l,2- benzisoxazol-3-yl)-l-pipéridinyl]éthyl]-6,7-dihydro-2-méthyl-4H-pyrido[l,2-a]- pyrimidin-4-one (II-b), et 3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-pipéridinyl]-éthyl]-6,7,8,9-tétrahydro-2-méthyl-9-pentadécyl-4H-pyrido[l,2-a]pyrimidin-4-one (III), et qui présente une dimension granulométrique moyenne comprise entre 20 et 150 ?m.