发明名称 |
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 |
摘要 |
<p>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.</p> |
申请公布号 |
WO2006114384(A1) |
申请公布日期 |
2006.11.02 |
申请号 |
WO2006EP61694 |
申请日期 |
2006.04.20 |
申请人 |
JANSSEN PHARMACEUTICA N.V.;SPITTAELS, THOMAS, FREDERIK, ERNESTINE;VAN DUN, JOANNES, PETRUS;VERBRAEKEN, JURGEN, ALOIS;WOUTERS, BENNY |
发明人 |
SPITTAELS, THOMAS, FREDERIK, ERNESTINE;VAN DUN, JOANNES, PETRUS;VERBRAEKEN, JURGEN, ALOIS;WOUTERS, BENNY |
分类号 |
C07D471/04 |
主分类号 |
C07D471/04 |
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