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Total Synthesis of Resiniferatoxin

Vasil H. Vasilev, Lukas Spessert, Kuan Yu, Thomas J. Maimone

2022Journal of the American Chemical Society31 citationsDOI

Abstract

From both structural and functional perspectives, the large family of daphnane diterpene orthoesters (DDOs) represent a truly remarkable class of natural products. As potent lead compounds for the treatment of pain, neurodegeneration, HIV/AIDS, and cancer, their medicinal potential continues to be heavily investigated, yet synthetic routes to DDO natural products remain rare. Herein we report a distinct approach to this class of complex diterpenes, highlighted by a 15-step total synthesis of the flagship DDO, resiniferatoxin.

Topics & Concepts

ChemistryResiniferatoxinHuman immunodeficiency virus (HIV)Total synthesisNatural productDiterpeneStereochemistryBiochemistryVirologyReceptorTransient receptor potential channelTRPV1BiologyBioactive Natural Diterpenoids ResearchPlant-based Medicinal ResearchPhytochemistry and Biological Activities
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