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The natural product cucurbitacin B has been widely studied because of its multiple biological activities, especially its potent antitumor effects. However, modifications of cucurbitacin B are mainly focused on the C2 and C16 site, studies on the C25 acetoxy group are still limited. We successfully developed a palladium‐catalyzed allylic coupling of cucurbitacin B with boronic acids, providing a one‐step...
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