Three-Component Synthesis of Benzhydrylamines from Arylzinc Halides

Significance

A simple method for the one-pot formation of tertiary benzhydrylamines from easily available aryl bromides, benzaldehydes and secondary amines is described. It is also an interesting example of a new three-component Mannich-type reaction. The used organozinc species are compatible with a broad variety of functional groups. The substituted benzhydrylamines which are formed in this reaction are some of the most widespread compounds for pharmacological use. Arylzinc bromides are prepared in situ via a cobalt-catalyzed insertion of Zn into aryl bromides. The overall reaction protocol is quite simple and practical.