Synlett 1995; 1995(6): 605-606
DOI: 10.1055/s-1995-5010
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The Ligand Effect in Copper(I)-Catalyzed Chemoselective Amide Carbamoylation in Cabergoline Synthesis

Ilaria Candiani, Walter Cabri, Franco Zarini, Angelo Bedeschi* , Sergio Penco
  • *Process Research, Pharmacia, Via Giovanni XXIII, 23, 20014 Nerviano (MI), Italy, Fax 39 2 583833
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Publication History

Publication Date:
31 December 2000 (online)

The effect of phosphorus and nitrogen ligands on the CuCl catalysed reaction of ethylisocyanate with an ergoline carboxamide has been studied. Phosphorus ligands afford chemoselectively the desired compound, while nitrogen ligands revert the observed selectivity. The use of phosphorus and nitrogen ligands is a novel and mild method for the Cu(I) salts catalyzed carbamoylation by alkylisocyanates.