Synthesis of hydrophospohoryl derivatives of the antifungal antibiotic pimaricin by the Kabachnik-Fields reaction

Reactions of the polyene macrolide antibiotic pimaricin with aromatic aldehydes and hypophosphorous acid are shown to afford pimaricin hydrophosphoryl derivatives. Physicochemical and biological properties of these compounds are explored. Biological studies indicated that the pimaricin hydrophosphoryl derivatives are low toxic agents possessing a high antifungal activity.