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A novel two step methodology for readily accessible natural “pulvinone” derivatives in excellent yields has been developed starting from activated precursors, bearing a functionalized 1,3-dioxolane-2,4-diones (OCA’s), as dually protected-activated synthons of α-hydroxy acids. The present procedure is based on a tandem C-acylation-cyclization process under mild conditions with good yields. Additionally, pulvinones show an important medicinal profile with the tetronate heterocycle exhibiting favorable pharmacokinetic (PK) and ADME-Tox properties that can be considered unexploited so far due to synthetic limitations.

A novel synthetic protocol for the synthesis of pulvinones, and naturally occurring Aspulvinone E , molecules of medicinal interest