A regioselective rhodium-catalyzed carboxylate-directed thiolation process was developed. Several benzoic-acid derivatives and disulfides were found to be well-tolerated, and they yielded the corresponding products in moderate to good yields. Compounds… Click to show full abstract
A regioselective rhodium-catalyzed carboxylate-directed thiolation process was developed. Several benzoic-acid derivatives and disulfides were found to be well-tolerated, and they yielded the corresponding products in moderate to good yields. Compounds such as the key precursor of roflumilast can be obtained via this reaction, thereby highlighting the potential of this synthetic approach.
               
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