发明授权
- 专利标题: 14-halo-camptothecins
- 专利标题(中): 14-halo-喜树碱
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申请号: US348452申请日: 1994-12-02
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公开(公告)号: US5459269A公开(公告)日: 1995-10-17
- 发明人: Daniel L. Comins
- 申请人: Daniel L. Comins
- 申请人地址: NC Raleigh
- 专利权人: North Carolina State University
- 当前专利权人: North Carolina State University
- 当前专利权人地址: NC Raleigh
- 主分类号: C07D213/64
- IPC分类号: C07D213/64 ; C07D491/04 ; C07D491/052 ; C07D491/22
摘要:
A method of making racemic DE ring intermediates for the synthesis of camptothecin and camptothecin analogs employing novel intermediates of Formula (XX) and (XXI): ##STR1## wherein R.sub.20 is loweralkyl, R is loweralkyl, Y is H or halogen, and R.sub.21 is loweralkoxy; as precursors to the DE ring intermediate.The present invention also provides a camptothecin analog of Formula (I-A): ##STR2## wherein: Hal is a halogen;and the remainder of the variables are as defined in the specification.Additionally, other novel compounds useful in the preparation of the compounds of Formula (I-A) and methods of producing compounds of (I-A) are also provided.
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