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In recent years the diterpene isosteviol, obtained via acid catalyzed rearrangement of stevioside, has gained growing interest by scientists. Its structural features and easy accessibility make isosteviol a useful starting material in organic synthesis. In this review, we group all existing modifications to the isosteviol moiety, ranging from biological transformation to rearrangements of the terpene skeleton. We will also discuss the known macrocycles based on isosteviol