Abstract
A one‐pot transition‐metal‐free selective iodoarylation of pyrazoles with aryliodine diacetates has been developed. The reaction proceeds via the generation of NH‐pyrazole‐iodonium salts in situ, followed by sequential phen/K2CO3‐mediated intermolecular arylation. When the iodonium ylide was directly used as substrate, the difunctionalization products could be prepared in high yield under base‐ and metal‐free conditions. This transformation provides an efficient route to high‐value multisubstituted pyrazole derivatives from simple and readily available substrates.
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