发明授权
US08093391B2 Process for the preparation of substantially pure palonosetron and its acid salts
失效
制备基本上纯粹的帕洛诺司琼及其酸式盐的方法
- 专利标题: Process for the preparation of substantially pure palonosetron and its acid salts
- 专利标题(中): 制备基本上纯粹的帕洛诺司琼及其酸式盐的方法
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申请号: US12652090申请日: 2010-01-05
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公开(公告)号: US08093391B2公开(公告)日: 2012-01-10
- 发明人: Sugata Chatterjee , Ajay Singh Rawat , Anil V. Pawar , Jetti Rajanikanth , Penigandla Venkateswarlu
- 申请人: Sugata Chatterjee , Ajay Singh Rawat , Anil V. Pawar , Jetti Rajanikanth , Penigandla Venkateswarlu
- 申请人地址: IN Gujarat
- 专利权人: Sterling Biotech Research Center
- 当前专利权人: Sterling Biotech Research Center
- 当前专利权人地址: IN Gujarat
- 代理机构: Barnes & Thornburg LLP
- 代理商 Mark J. Nahnsen
- 优先权: IN1677/MUM/2009 20090721
- 主分类号: C07D401/00
- IPC分类号: C07D401/00 ; C07D211/06 ; C07D211/40 ; C07D211/54 ; C07D211/00 ; A61K31/44 ; A61K31/445 ; A01N43/40
摘要:
This invention relates to an improved and scalable process for the preparation of substantially pure palonosetron and its acid addition salts, in particular hydrochloride (I) which comprises of, (a) converting intermediate (IIa) as such or as its freebase (II) to a crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) via hydrogenation under pressure with an appropriately chosen hydrogenation catalyst in an suitable organic solvent. (b) making the resulting crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) substantially free from (II) or (IIa) via halogenation reaction. (c) Finally, converting the resulting diastereomeric palonosetron (VIII) or its hydrochloride (VIIIa) substantially free from intermediate (II) or (IIa) to the desired palonosetron hydrochloride (I) in substantially pure form via selective crystallization from a suitable single or mixture of organic solvents.