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An eight-step gram-scale synthesis of (-)-jiadifenolide
Hai-Hua Lu1, Michael D Martinez1, Ryan A Shenvi1
1Department of Chemistry, The Scripps Research Institute, La Jolla, California 92037, USA.
Abstract:
Development of a biologically active secondary metabolite into a useful medicine requires continuous access to meaningful quantities of material. Although any chemical synthesis is broadly useful for its versatility, identification of a synthesis route that can be economically scaled represents a greater challenge. Here we report a concise synthesis of the neurotrophic trace metabolite (-)-jiadifenolide and its production on a gram-scale. The brevity of the route and the structural similarity of a key intermediate to many potent Illicium terpenes make chemical synthesis the unquestionable method for accessing and modifying these potential therapeutics.