| 摘要 |
The invention comprises compounds of the formula <FORM:1095833/C2/1> wherein R is hydrogen or an aryl-substituted C1- 5 alkyl-CO-, aryl-CO-, halo-substituted C1- 5 alkyl-CO-, or cyano-substituted C1- 5 alkyl-CO-group and R1 is a C1-5 alkyl, H.CO- or C1- 5 alkyl-CO- group and acid addition salts thereof and a process for the preparation of compounds of the above formula wherein R may in addition be hydrogen or a C1- 5 alkyl-CO- or H.CO-group which comprises selectively hydrolysing the corresponding acetyl compound (R = CH3CO), e.g. vincaleukoblastine or leurochristine to give a compound wherein R and possibly also R1 are hydrogen, acylating, e.g. by treating with an acid anhydride R112O, where R11 is HCO, C1- 5 alkyl-CO, aryl-substituted C1- 5 alkyl-CO, aryl-CO, halo-C1- 5 alkyl-CO or cyano-C1- 5 alkyl-CO, to give a mixture of mono- and di-acylated products and selectively hydrolysing, e.g. by treatment with silica gel in moist methanol. The first hydrolysis step to remove the acetyl group may be carried out with methanolic HCl, hydrazine hydrate in ethylene glycol or ethanol, potassium carbonate in methanol or with one equivalent of potassium hydroxide in methanol. Pharmaceutical preparations for the treatment of leukemia comprise the above compounds of the invention and an excipient.
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