WERKWIJZE VOOR HET BEREIDEN VAN ANTI-TUMORMIDDELEN EN DAARVOOR GESCHIKTE GENEESKRACHTIGE VERBINDINGEN.

摘要

The process for the preparation of daunomycin and of 4'-epi-daunomycin and the corresponding ss anomers comprises reacting daunomycinone with a 1-chloro-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxyhexose which has the L-lyxo or L-arabino configuration in an organic solvent in the presence of a mercury salt as catalyst and of a hydrogen chloride acceptor and then removing the trifluoroacetyl protective groups in the glycoside compounds which are formed, and separating the alpha and ss anomers. The compounds display excellent biological properties as potent inhibitors of cell mitosis and proliferative activity in cultured cells in vitro.