METHOD FOR THE PREPARATION OF STRICTOZIDIN

摘要

1. Method for the preparation of strictosidine of the formula (I) see diagramm : EP0156267,P5,F3 by condensing secologanin of formula (II) see diagramm : EP0156267,P5,F5 and tryptamine of formula (III) see diagramm : EP0156267,P6,F1 in an aqueous solution, characterised in that the tryptamine is used in a molar ratio of (20-80) : (80-20), advantageously in a molar ratio of 50 : 50, as a mixture of the free tryptamine base and a salt of tryptamine formed with a mineral acid, and to the aqueous solution is added an additional protonic solvent, preferably acetic acid, in a quantity which at least ensures dissolution of the whole quantity of the tryptamine base, but comprises not more than 5 wt.% of the reaction mixture, and the resulting vincoside lactam of formula (IV) see diagramm : EP0156267,P6,F2 is precipitated by filtration, and the strictosidine isolated in a known manner.