Abstract
A mono- N-protected amino acid (MPAA) ligand promoted, Pd(II)-catalyzed C(sp2)-H arylation of free primary 2-phenylethylamines using the native NH2 as the directing group has been achieved. This method is compatible with challenging simple primary 2-phenylethylamines bearing α-hydrogen atoms. Application of this protocol in the direct structure modification of the drug molecule amphetamine is also demonstrated.
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