Abstract
Reductive alkylation is a practical route for a total synthesis of regioisomers of spider toxin JSTX-3, a polyamine amide which is a selective glutamate receptor antagonist and may have potential as a neuroprotective agent. The strategy is based upon a reductive alkylation step which enables one free araine to be generated regiospecifically in the new polyamine, or the regiospecific incorporation of a hexahydropyrimidine moiety which conformationally restricts the polyamine amide backbone.
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