Process for the preparation of new vinblastine cytostatic...

C - Chemistry – Metallurgy – 07 – D

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260/237.3

C07D 519/04 (2006.01)

Patent

CA 1174672

Abstract The invention relates to a process for the preparation of new cyto- static compounds and pharmaceutical compositions containing them More particu-larly, the invention concerns a process for preparing compounds of the general formula (1) Image (I) in which R4 is a .beta.-hydroxyl and R3 is an .alpha.-ethyl; or R4 is hydrogen and R3 is a .beta.-ethyl; R41 is a straight chained alkyl having from 1 to 10 carbon atoms, other than ethyl or a branched chained alkyl having fro 3 to 10 carbon atoms, in which the carbon atom attached to the ?Na-CH2-O- group has a primary or secondary configuration or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety; R1 is methoxy and R2 is acetyl. The pharmaceutical compositions comprising as active ingredient pharmaceutically effective amounts of said compounds are also within the scope of the invention.

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