This review highlights recent strategies for forming C–S bonds, enhancing natural product synthesis for therapeutic uses.
Sulfur imparts distinctive reactivity, conformational bias, and redox versatility to natural products, giving rise to potent antibacterial, antiviral, anticancer, and enzyme-inhibitory activities. Over the past five years, highly regio- and stereoselective C–S bond-forming strategies have enabled concise access to increasingly complex sulfur frameworks. This review surveys representative total syntheses reported from March 2020 to January 2024, grouped by sulfur functionality—thioethers, disulfides, sulfoxides, thioacetals, thiazoles, thiazolines, and isothiazolinones—and shows how these advances shorten step counts, facilitate late-stage diversification, and provide a foundation for rapid structure–activity relationship studies of sulfur-rich scaffolds poised for therapeutic development.
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Lee et al. (2025) studied this question.
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