Ginkgolides are complex polyoxygenated diterpenoids isolated from the leaves and root bark of the ginkgo biloba tree, also known as the maidenhair tree or as the "Living Fossil" as its fossils date back to the Jurassic period (170M years) (Figure ). Ginkgolides A (1), B (2), C (3) and M (4) (for minor) were first isolated by Furukawa in 1932 and their structures were subsequently elucidated in 1967 by Nakanishi. In 1987, Weinges et al. discovered, isolated and characterized ginkgolide J (5). More recently, the Wang and Peng groups independently isolated ginkgolides K, L, P and Q. Ginkgolides, especially ginkgolide B (2), are strong antagonists to the platelet-activating factor (PAF) receptor (PAFR) which is known as a potent inflammatory factor that plays a role in acute and chronic inflammation. It has been also reported that ginkgolides could serve as effective therapies against central nervous system illnesses such as Alzheimer's and Parkinson's disease, multiple sclerosis and it is also useful in migraine prophylaxis. The compact and highly oxygenated polycyclic molecular structure of ginkgolides including six 5-membered rings, two adjacent quaternary carbon centers and an unusual tert-butyl group. Although their therapeutic profile is remarkable, their daunting structures present a significant challenge for chemical synthesis, for which only a handful of synthetic studies of these molecules have been performed, 11 including the total syntheses of ginkgolide A (1) and B (2) by the groups of Corey 12 and Crimmins. To the best of our knowledge, there are no reports for the total synthesis of ginkgolide C (3), the most complex diterpene of the family, which bears 12 contiguous stereocenters, and eleven oxygenated carbons. This diterpene would provide a unique synthetic platform for the advancement of new strategies and methods. Herein, we report the first total synthesis of (±)-ginkgolide C (3) as well as the formal syntheses of (±)-ginkgolide A ( ) and (±)-ginkgolide B (2).