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Preparation of N-arylpiperazines and other N-aryl compounds from aryl bromides as scaffolds of bioactive compounds


 

M. Romero, Y. Harrak, J. Basset, L. Ginet, P. Constans, and M.D. Pujol. Preparation of N-arylpiperazines and other N-aryl compounds from aryl bromides as scaffolds of bioactive compounds. Tetrahedron, 62, 9010-9016 (2006).

Abstract
Aryl bromides are coupled with N-compounds to give the corresponding arylamines in the presence of a palladium catalyst, a suitable ligand, and a weak base. The catalysts perform well for a large number of different starting material combinations at 100-150 °C with drops of toluene or without solvent, and with low catalyst levels (0.12 mol % Pd). The low catalyst amount makes the process environment friendly.

Keywords
N-Arylpiperazines, N-Arylindoles, Substituted anilines, Palladium catalyst, N-Arylation, Aryl halides.

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