Pharmachemie B.v.

Eric Wilhelmus Damen

Dick De Vos

Johan W Scheeren

Hidde J Haisma

Ruben G Leenders

Pieter H Houba

10-Deacetylbaccatin III is selectively acylated to baccatin III and derivatives thereof in high yield with anhydrides (e.g. acetic anhydride), catalysed by Lewis acids. Extremely effective catalysts in this reaction are compounds of the formula ML.sub.x wherein M is a rare earth metal and L is a anion, preferably a strong electron withdrawing counterion such as triflate.

Method for the preparation of baccatin III and derivatives thereof from

Anthracycline derivatives are disclosed which are coupled to an enzymatically cleavable N-phenyl-O-glycosyl carbamate spacer group, which derivatives are represented by the formula ##STR1## as well as the acid addition salts thereof. Further the synthesis of these derivatives and their use, alone or in combination with enzymes or antibody enzyme conjugates are disclosed.

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Nijmegen, Netherlands

Eric Wilhelmus Damen