One-pot synthesis of pharmacologically active diamines via rhodium-catalysed carbonylative hydroaminomethylation of heterocyclic allylic amines

Abstract

Pharmacologically active derivatives of phenothiazine, iminodibenzyl, carbazole and pyrazole are prepared with high yields and chemoselectivity by the reaction of the correspondingN-allylic orN-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. [Display omitted]