Xu, Hai-Feng; Pan, You-Lu; Li, Gang-Jian; Hu, Xu-Yang; Chen, Jian-Zhong published the artcile< Copper(II)-Catalyzed Direct C-H (Hetero)arylation at the C3 Position of Indoles Assisted by a Removable N,N-Bidentate Auxiliary Moiety>, Electric Literature of 329214-79-1, the main research area is arylated indole regioselective preparation; indole arylboronic ester arylation copper catalyst.
The regioselective arylation of inert C3-H bonds in indoles reacting with arylboronates via effective copper-mediated catalysis with the aid of a facile and removable 2-pyridinylisopropyl (PIP) group without ligand participation was reported. This newly established method features high compatibility with diverse functional groups between coupling partners, including both indole substrates and arylboron reagents, consequentially leading to operational simplicity and providing access to generate the desired arylated products I [R = H, 4-Me, 5-MeO, 6-Br, etc.; R1 = Me, Bn; Ar = Ph, 2-thienyl, 3-pyridyl, etc.] in good to excellent yields of up to 97%. Synthetically, the PIP-derived amide moiety could subsequently be readily removed under mild reaction conditions to produce useful indolecarboxylic acids for further transformation.
Journal of Organic Chemistry published new progress about Amides, secondary Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Electric Literature of 329214-79-1.