No abstract

Reported herein is an unprecedented protocol for trifluoromethylation of unactivated aliphatic C(sp3)−H bonds. With Cu(OTf)2 as the catalyst, the reaction of N‐fluoro‐substituted carboxamides (or sulfonamides) with Zn(CF3)2 complexes provides the corresponding δ‐trifluoromethylated carboxamides (or sulfonamides) in satisfactory yields under mild reaction conditions. A radical mechanism involving 1,5‐hydrogen atom transfer of N‐radicals followed by CF3‐transfer from CuII−CF3 complexes to the thus formed alkyl radicals is proposed.

Sulfones are not only important structural motifs in pharmaceuticals and agrochemicals but also versatile intermediates in organic synthesis. However, C(sp 3 )-sulfonyl bond formations remain underdeveloped. In this issue of Chem, Li and co-workers demonstrate that the merger of photo-organocatalysis and copper-catalysis enables the decarboxylative radical sulfonylation with organosulfinates at room temperature under redox-neutral conditions. The method leads to the improved synthesis of anti-prostate cancer drug bicalutamide and should find more important applications in drug discovery.