01525nas a2200241 4500008004100000022001400041245011600055210006900171260000900240300001400249490000800263520072100271653001400992653001901006653002501025653001101050653001101061653001701072100002201089700002301111700002001134856012901154 2020 eng d a1615-415000aCopper-catalyzed direct arylation of indoles and related (hetero)arenes: a ligandless and solvent-free approach0 aCoppercatalyzed direct arylation of indoles and related heteroar cJUN  a2534-25400 v3623 a

A ligandless and solvent-free copper-catalyzed method for the regioselective C-H bond arylation of indoles and related heteroarenes is reported. The use of CuCl efficiently catalyzes the direct coupling of diverse heteroarenes with aryl iodides via chelation-assistance. This reaction could tolerate sensitive and structurally diverse functionalities, including halides, ethers, thioethers, amines, indolyl, pyrrolyl and carbazolyl groups. The directing group, 2-pyridinyl can be smoothly removed to generate C-2 arylated free-NH indoles, and the arylated indoles can further be functionalized into Tryptamine derivatives. Preliminary mechanistic study revealed a radical pathway for the arylation reaction.

10aArylation10aC-H activation10aChelation-assistance10aCopper10aIndole10aSolvent-free1 aPandey, Dilip, K.1 aShabade, Anand, B.1 aPunji, Benudhar uhttps://library.ncl.res.in/content/copper-catalyzed-direct-arylation-indoles-and-related-heteroarenes-ligandless-and-solvent