发明公开
EP2861554A2 IMPROVED PROCESS FOR THE PREPARATION OF TREPROSTINIL AND DERIVATIVES THEREOF
审中-公开
VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON TREPROSTINIL UND DATEIVATEN DAVON
- 专利标题: IMPROVED PROCESS FOR THE PREPARATION OF TREPROSTINIL AND DERIVATIVES THEREOF
- 专利标题(中): VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON TREPROSTINIL UND DATEIVATEN DAVON
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申请号: EP13724809.2申请日: 2013-05-22
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公开(公告)号: EP2861554A2公开(公告)日: 2015-04-22
- 发明人: JAIN, Nareshkumar F. , KIRKUP, Michael P. , MARELLA, Michael A. , GHONE, Sanjeevani, A.
- 申请人: SciPharm SàRL
- 申请人地址: 26-28, rue Edward Steichen 2540 Luxembourg LU
- 专利权人: SciPharm SàRL
- 当前专利权人: SciPharm SàRL
- 当前专利权人地址: 26-28, rue Edward Steichen 2540 Luxembourg LU
- 代理机构: Loidl, Manuela Bettina
- 优先权: US201261650836P 20120523; EP12172191 20120615
- 国际公布: WO2013174848 20131128
- 主分类号: C07C67/29
- IPC分类号: C07C67/29 ; C07C69/18 ; C07F7/18 ; C12P41/00 ; C07C47/565 ; C07C47/575 ; C07C51/377 ; C07C59/72
摘要:
A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.
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