发明授权
US06649778B1 Methods of preparing amino acid taxane derivatives and polymer conjugates containing the same
失效
制备氨基酸紫杉烷衍生物和含有它们的聚合物共轭物的方法
- 专利标题: Methods of preparing amino acid taxane derivatives and polymer conjugates containing the same
- 专利标题(中): 制备氨基酸紫杉烷衍生物和含有它们的聚合物共轭物的方法
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申请号: US10252024申请日: 2002-09-20
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公开(公告)号: US06649778B1公开(公告)日: 2003-11-18
- 发明人: Hong Zhao , Richard B. Greenwald
- 申请人: Hong Zhao , Richard B. Greenwald
- 主分类号: C07D30514
- IPC分类号: C07D30514
摘要:
Methods of preparing amino acid-substituted taxanes such as: using selected blocked amino acids are disclosed. After coupling of the blocked amino acid to the taxane, deprotection is carried out with about an equimolar amount of a secondary amine thus substantially avoiding base-catalyzed hydrolysis of amino acid from the taxane. The preferred amino acid-taxanes are useful as intermediates in the production of polymer conjugated therapeutic compositions or as part of pharmaceutically acceptable formulations.
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