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US 11,028,094 B2Granted
Preparative scale conversion of gonyautoxins to neosaxitoxin
OwnerAndrew Ian Selwood, Roelof Van Ginkel +1inventors
InventorsAndrew Ian Selwood, Roelof Van Ginkel, Craig Alan Waugh
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Abstract
A method of preparing neosaxitoxin in quantities of a purity sufficient to allow the compound to be used as an active pharmaceutical ingredient (API) is described. The method includes the reductive desulfonation of an unresolved mixture of gonyautoxin 1 (GTX1) and gonyautoxin 4 (GTX4).
Claims8
A method of preparing a quantity of purified neoSTX comprising:
- (a) contacting in solution at a pH in the range 7.2 to 7.8 a quantity of GTX1,4 and a quantity of a dithiol at a temperature and for a time sufficient to provide a conversion product in which greater than 97.5% (w/w) of the quantity of GTX1,4 has been converted to neoSTX;
- and then
- (b) applying the conversion product to a weak cation exchange sorbent and eluting with an aqueous weak acid to separate neoSTX from the dithiol and provide the quantity of purified neoSTX.
Dependencies are inferred from the claim text.