Copper(I)‐catalyzed radical 1,2‐benzylarylation of N‐phenethylenamides was developed and 1,1‐disubstituted N‐acyl tetrahydroisoquinolines were obtained in moderate to good yields. In this process, two new C–C bonds were formed in one‐step fashion with high atom economy. A possible reaction pathway for the formation of the products is also discussed.
The regioselectivity of radical addition and cyclization reaction of tertiary enamides between 5-membered benzoyl group and 5/6/7-membered benzyl group ring closure was investigated, and trifluoroethyl -containing N-Acyl isoindolines, N-acyl tetrahydro-isoquinolines, and N-benzoyl tetrahydro-1H-benzo[c]azepine were obtained in moderate to good yields with high atom economy. Possible reaction pathway for the formation of the products was also discussed in this paper.
A radical trifluoromethylation reaction of tertiary enamides was investigated and trifluoromethyl-containing isoindolinones were prepared under mild conditions. Using TMSCF 3 as a radical source, PhI(OAc) 2 as an oxidant and KHF 2 as an additive, tertiary enamides were converted to isoindolinones via a cascade addition and cyclization process in moderate to good yields.In recent years, triuoromethyl-containing azaheterocycles have attracted much attention for their potential application in the elds of pharmaceutical and agricultural chemistry.
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