Abstract: Natural products play a pivotal role in the advancement of state-of-the-art pharmaceuticals. To augment their therapeutic efficacy, structural modifications of these compounds are routinely performed. In this study, we introduce an efficient and environmentally benign electrochemical oxidative method for site-selective direct C-H activation of the Tanshinone IIA. This process is conducted under metal-free, oxidant-free, and base-free conditions. The reaction exhibits excellent functional group compatibility and retains high yields in large-scale operations, producing moderate to excellent yields of the desired Tanshinone IIA derivatives. Biological activity assays demonstrate that the compound 2h, 2s and 2o possesses superior antitumor efficacy compared to Tanshinone IIA.

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