Preparation of Aseptic 3-[2-[4-((6-Fluoro-1,2-Benzisoxazol-3-Yl)-1-Piperidinyl]-6,7,8,9-Tetrahydro-9-Hydroxy-2-Methyl-4H-Pyrido[1,2-a]Pyrimidin-4-One Palmitate Ester

Preparation of Aseptic 3-[2-[4-((6-Fluoro-1,2-Benzisoxazol-3-Yl)-1-Piperidinyl]-6,7,8,9-Tetrahydro-9-Hydroxy-2-Methyl-4H-Pyrido[1,2-a]Pyrimidin-4-One Palmitate Ester

The present invention concerns a process for preparing aseptic crystalline 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 palmitate ester (I) substantially free of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidi...

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Bibliographische Detailangaben
Hauptverfasser: VAN DUN JOANNES PETRUS, VERBRAEKEN JURGEN ALOIS, SPITTAELS THOMAS FREDERIK ERNESTINE, WOUTERS BENNY
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:The present invention concerns a process for preparing aseptic crystalline 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 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-1,2-benzisoxazol-3 -yl)-1-piperidinyl]ethyl]-6,7-dihydro-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (II-b), and 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-ethyl]-6,7,8,9-tetrahydro-2-methyl-9-pentadecyl-4H-pyrido[1,2-a]pyrimidin-4-one (III), and having an average particle size ranging from 20 to 150 mum.