Enantioselective Total Synthesis of Ginkgolide Derivatives Lacking the tert-Butyl Group, an Essential Structural Subunit for Antagonism of Platelet Activating Factor

Article abstract of DOI:10.1016/S0040-4039(00)92265-2

An enantioselective total synthesis of the ginkgolide B analog 3 is reported along with results of bioassays for antagonism of platelet activating factor.The three orders of magnitude difference in bioactivity of 2 and 3 demonstrates that the tert-butyl group of the ginkgolides is essential for anti-PAF potency.