(Beijing University of Chemical Technology, 2007) Hiji, Morris Frank; Zheng, GuoJun; Yuan, QiPeng
The new pathway for the synthesis of 2, 3-dichlorophenylpiperazine from cheap raw material, 2, 3-dichloroaniline is presented. The hydrogen sulphate salt of 2, 3-dichloroaniline was converted to the corresponding Aryl Iodide in good yield of 81 % by reacting with conc. H2SO4 and NaNO2 to form intermediate diazonium salt, which was further displaced by Kl. The desired product was obtained by reacting Aryl Iodide and piperazine in the presence of CuI as catalyst, proline as ligand,
K2C03 as base and dimethyl sulfoxide as solvent with yield of 20 % . The method is simple, utilizes cheap catalyst and ligand, insensitive to moisture; it is easy to separate the product, and can undergo large-scale production.