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Experimental study demonstrates copper-mediated C–H thiolation in free benzylamines, highlighting an affordable and sustainable transient directing group strategy for C–S bond formation.
A copper-mediated C–H thiolation reaction of benzylamines has been developed using a transient directing group strategy. In this reaction, picolinaldehyde was used as the catalyst, which forms a transient imine directing group in situ with benzylamines to facilitate C–H activation. This method not only provides a straightforward route to aryl sulfides but also represents one of the rare examples of first-row transition metal-mediated C–H functionalization via a transient directing group approach. The work highlights the potential of cost-effective copper catalysts in enabling challenging C–S bond formations, advancing the field of sustainable C–H functionalization.
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Mei et al. (2025) studied this question.
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