Radiolabeling of Siamenoside I with Carbon-14

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The synthesis of radiolabeled [25- 14 C]-siamenoside I following a synthetic route developed using unlabeled materials is disclosed. The synthesis features an early stage labeling of the mogrol’s C25 via an oxidative cleavage–reconstruction strategy and regioselective glycosylations directed by protecting group manipulations. This route provided access to adequate amounts of [25- 14 C]-siamenoside I for in vivo ADME and PK studies.