发明申请
US20140073787A1 PREPARATION OF 3-[2-[4-((6-FLUORO-1, 2-BENZISOXAZOL-3-YL)-L-PIPERIDINYL)-6, 7, 8, 9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO[ 1, 2-A]-PYRIMIDIN-4-ONE (PALIPERIDONE) AND PALIPERIDONE PALMITATE.
审中-公开
制备3- [2- [4 - （（6-氟代-1,2-苯并恶唑-3-基）-L-哌啶子基）-6,7,8,9-四氢-9-羟基-2-甲基 - 4H-吡啶并[1,2-A] - 嘧啶-4-酮（PALIPERIDONE）和PALIPERIDONE PALMITATE。
![PREPARATION OF 3-[2-[4-((6-FLUORO-1, 2-BENZISOXAZOL-3-YL)-L-PIPERIDINYL)-6, 7, 8, 9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO[ 1, 2-A]-PYRIMIDIN-4-ONE (PALIPERIDONE) AND PALIPERIDONE PALMITATE.](/docs/US/2014-03-13/US20140073787A1/abs.jpg.600x600.jpg)
- 专利标题： PREPARATION OF 3-[2-[4-((6-FLUORO-1, 2-BENZISOXAZOL-3-YL)-L-PIPERIDINYL)-6, 7, 8, 9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO[ 1, 2-A]-PYRIMIDIN-4-ONE (PALIPERIDONE) AND PALIPERIDONE PALMITATE.
- 专利标题（中）： 制备3- [2- [4 - （（6-氟代-1,2-苯并恶唑-3-基）-L-哌啶子基）-6,7,8,9-四氢-9-羟基-2-甲基 - 4H-吡啶并[1,2-A] - 嘧啶-4-酮（PALIPERIDONE）和PALIPERIDONE PALMITATE。
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申请号： US13819372申请日： 2012-05-30
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公开(公告)号： US20140073787A1公开(公告)日： 2014-03-13
- 发明人: Ramamohan Rao Davuluri , Ravi Ponnaiah , Praveen Kumar Neela , Guruswamy Batthini , Telagareddy Venkata Narasimharao , Kosireddy Ravanababu , Kallepally Sudheer
- 申请人： Ramamohan Rao Davuluri , Ravi Ponnaiah , Praveen Kumar Neela , Guruswamy Batthini , Telagareddy Venkata Narasimharao , Kosireddy Ravanababu , Kallepally Sudheer
- 优先权： IN184/CHE/2011 20110531
- 国际申请： PCT/IN2011/000375 WO 20120530
- 主分类号： C07D471/04
- IPC分类号： C07D471/04
![PREPARATION OF 3-[2-[4-((6-FLUORO-1, 2-BENZISOXAZOL-3-YL)-L-PIPERIDINYL)-6, 7, 8, 9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO[ 1, 2-A]-PYRIMIDIN-4-ONE (PALIPERIDONE) AND PALIPERIDONE PALMITATE.](/abs-image/US/2014/03/13/US20140073787A1/abs.jpg.150x150.jpg)
摘要：
An improved process for the synthesis of 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 (Paliperidone) and Paliperidone Palmitate through a novel intermediate (2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido [1,2-a]pyrimidine-4-one Palmitate ester.
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