A novel, efficient and eco‐friendly synthetic strategy for the preparation of thiosulfonates by electrochemical oxidation of thiols is presented. This method enabled thiosulfonates formation under catalyst‐ and oxidant‐ free conditions. The electrochemical oxidizing reaction exhibits a good functional group compatibility and broad scope, hence, providing accesses to various disulfides (31 examples) and thiosulfonates (23 examples). The reactions proceeded under simple and mild reaction conditions, and could be scaled up to the gram‐scale. They are also applicable in the late‐stage synthesis of bioactive molecules.

Ibuprofen is one of the most potent non-steroid anti-inflammatory drugs (NSAIDs) and plays an important role in the treatment of neurodegenerative diseases. However, its poor brain penetration and serious side effects at therapeutic doses, has hindered its further application. Thus, it is of great interest to develop a carrier-mediated transporter (CMT) system that is capable of more efficiently delivering ibuprofen into the brain at smaller doses to treat neurodegenerative diseases. In this study, a dual-mediated ibuprofen prodrug modified by glucose (Glu) and vitamin C (Vc) for central nervous system (CNS) drug delivery was designed and synthesized in order to effectively deliver ibuprofen to brain. Ibuprofen could be released from the prepared prodrugs when incubated with various buffers, mice plasma and brain homogenate. Also, the prodrug showed superior neuroprotective effect in vitro and in vivo than ibuprofen. Our results suggest that chemical modification of therapeutics with warheads of glucose and Vc represents a promising and efficient strategy for the development of brain-targeting prodrugs by utilizing the endogenous transportation mechanism of the warheads.

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The chemosynthetic approach was skillfully combined with a GOx-enabled tumor survival microenvironment deteriorating strategy to achieve secure and satisfactory tumor ablation through multimodal synergistic starvation/oxidation/chemotherapy.

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