Invention Grant
US08269007B2 Crystalline form II of 7-(dimethoxy-methyl) camptothecin, its use as intermediate and products obtained therefrom
有权
7-(二甲氧基 - 甲基)喜树碱的结晶形式II,其用作中间体和由其获得的产物
- Patent Title: Crystalline form II of 7-(dimethoxy-methyl) camptothecin, its use as intermediate and products obtained therefrom
- Patent Title (中): 7-(二甲氧基 - 甲基)喜树碱的结晶形式II,其用作中间体和由其获得的产物
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Application No.: US12670905Application Date: 2008-07-22
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Publication No.: US08269007B2Publication Date: 2012-09-18
- Inventor: Walter Cabri , Mauro Marzi , Fabrizio Giorgi , Elena Badaloni , Silvia Armaroli , Giuseppe Marazzi
- Applicant: Walter Cabri , Mauro Marzi , Fabrizio Giorgi , Elena Badaloni , Silvia Armaroli , Giuseppe Marazzi
- Applicant Address: IT Rome
- Assignee: Sigma-Tau Industrie Farmaceutiche Riunite SpA
- Current Assignee: Sigma-Tau Industrie Farmaceutiche Riunite SpA
- Current Assignee Address: IT Rome
- Agency: Lucas & Mercanti, LLP
- Priority: EP07113597 20070801
- International Application: PCT/EP2008/059597 WO 20080722
- International Announcement: WO2009/016068 WO 20090205
- Main IPC: C07D491/22
- IPC: C07D491/22 ; C07D491/147

Abstract:
This invention relates to a process for preparing a crystalline form of (4S)-11(dimethoxymethyl)-4-ethyl-4-hydroxy-1H-pyrano[3′4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, also named 7-(dimethoxy-methyl)camptothecin). With the provision of a particular crystallization step, in appropriate way, a new crystalline form of the above compound is obtained. The process for the preparation of the polymorph Form II comprises transforming camptothecin to the corresponding 7-(dimethoxy-methyl)-camptothecin, and crystallizing from methanol.
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