Aryl- and heteroarylamines are essential intermediates in the manufacturing of pharmaceuticals and agrochemicals. These arylamines can be conveniently accessed by the Pd-catalyzed arylation of ammonia; however, avoiding the subsequent arylation is difficult. We have synthesized new biaryl phosphine ligands, Me3(OMe)XPhos (L1)  and Me3(OMe)PhXPhos (L2  ), which, in combination with the Pd-precatalyst to form 1a  and 1b , respectively, can efficiently promote the cross-coupling of ammonia with various aryl and heteroaryl halides, selectively affording the corresponding aryl- and heteroarylamines under milder conditions (eq 1).

Improved selective protocol for the palladium-catalyzed arylation of ammonia to arylamines and heteroarylamines under mild conditions

245th National Meeting (2013)

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