One-pot synthesis of pharmacologically active diamines via rhodium- catalysed carbonylative hydroaminomethylation of heterocyclic allylic amines
Pharmacologically active derivatives of phenothiazine, iminodibenzyl, carbazole and pyrazole are prepared with high yields and chemoselectivity by the reaction of the corresponding N-allylic or N-methallylic compounds, primary or secondary amines, carbon monoxide and hydrogen in the presence of [Rh(cod)Cl]2 as catalyst via a one pot hydroformylation - amine condensation - reduction sequence.
Rische, Thorsten,Mueller, Kai-Sven,Eilbracht, Peter