发明授权
- 专利标题: Method for the preparation of 9-amino camptothecin
- 专利标题(中): 9-氨基喜树碱的制备方法
-
申请号: US602792申请日: 1996-09-30
-
公开(公告)号: US5840899A公开(公告)日: 1998-11-24
- 发明人: Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini
- 申请人: Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini
- 申请人地址: ITX Milan
- 专利权人: Pharmacia S.p.A.
- 当前专利权人: Pharmacia S.p.A.
- 当前专利权人地址: ITX Milan
- 优先权: GBX9410388 19940524
- 主分类号: C07D491/22
- IPC分类号: C07D491/22
摘要:
9-Amino camptothecin of formula (I) ##STR1## is prepared by: 1) reducing a compound of formula (II): ##STR2## wherein Hal is 10- or 12-halogen, in a single step to the 9-amino-camptothecin of formula (I) or, alternatively, 2a) reductively removing the Hal group from a compound of formula (II) so obtaining the compound of formula (III): ##STR3## and 2b) reducing the compound of formula (III) so obtaining the 9-amino camptothecin of formula (I); the said steps 1 and 2a) and, optionally, step 2b) each being carried out in the presence of a catalytic amount of a compound of formula PdL.sub.2 wherein L is acetate or halogen and, additionally, in the presence of an ammonium formate as a hydrogen source. The 9-amino camptothecin of formula (I) is useful as inhibitor of the enzyme topoisomerase I. It is useful in the treatment of cancers, in particular leukaemia, colon and rectal tumours.
公开/授权文献
- US5085939A Thin film-coated polymer webs 公开/授权日:1992-02-04