Halo-Substituted Aminobenzenes Prepared by Pd-Catalyzed Amination

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Abstract
The selective monoamination of aryl dihalides by primary amines and polyamines in the presence of the Pd2(dba)3/dppf catalytic system and NaOt-Bu provides a convenient method for the synthesis of aminobenzenes substituted at the ortho, meta, or para position of the aryl ring by a halogen atom. Under these conditions the reaction of polyamine compounds having 1,2-diaminoethane or 1,3-diaminopropane moieties proceeds selectively leading to monoaryl-substituted derivatives of polyamines. Moreover, this is a remarkably efficient method to realize the arylation of a primary amine group of polyamines in the presence of a secondary one.

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