| abstract |
The present invention relates to a process for the preparation of water-soluble camptothecin derivatives of formula (I) and pharmaceutically acceptable salts thereof, and to pharmaceutical compositions containing them. In formula (I), n is 1 or 2, and i) R 1 and R 2 are independently hydrogen, C 1-6 alkyl or hydroxy (C 1-6 alkyl), ii) R 1 is hydrogen and R 2 is -COR 3 in general. wherein R3 is perhalo (C1-6 alkyl), or iii) R1 and R2 together form a nitrogen atomazetidine, pyrrolidine, piperidine, morpholine, thiomorpholine or piperazine ring which is optionally N-substituted with 1-6 carbon atoms. C 6 -C 6 alkyl or phenyl or phenyl substituted by one or more perhalo- (C 1-6 alkyl) or C 1-6 alkoxy groups, or -COR 5 wherein R 5 is C 1-6 alkoxy. ŕ |