| 摘要 |
PCT No. PCT/EP95/01692 Sec. 371 Date Sep. 30, 1996 Sec. 102(e) Date Sep. 30, 1996 PCT Filed May 4, 1995 PCT Pub. No. WO95/32207 PCT Pub. Date Nov. 30, 19959-Amino camptothecin of formula (I) <IMAGE> (I) is prepared by: 1) reducing a compound of formula (II): <IMAGE> (II) 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): <IMAGE> (III) 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 PdL2 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. |
