Abstract
AbstractTimefurone (1), a methyl thioether analogue of khellin (2), was labeled with tritium at the C‐2 position and with carbon‐14 at the C‐5 position for conducting in vivo biotransformation studies with 1. Tritium labeled 1 was prepared by lithiating and tritiating a silyllated derivative of khellinone (3) at C‐2, followed by converting the labeled khellinone into 1. Carbon‐14 labeled 1 was obtained by first dismantling the pyrone ring of khellin, followed by reconstruction of the ring with incorporation of carbon‐14 into the carbonyl position.
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