RAPID SYNTHESIS OF ALIPHATIC AMIDES BY REACTION OF CARBOXYLIC-ACIDS, GRIGNARD-REAGENT AND AMINES - APPLICATION TO THE PREPARATION OF [C-11]AMIDES

Aliphatic amides have been prepared in moderate to good yields (30-70% ) by treatment in THF of magnesium halide carboxylates with amines in the presence of 2.5 equivalents of alkylmagnesium halide. The reaction is rapid (<30 min) and has been successfully applied to the synthesis of amides labelled with carbon-ii (beta(+), t(1/2): 20.4 min). [C-11] Aliphatic amides have been obtained in 15-60% radiochemical yields [de cay corrected to end of bombardment (EOB), 5 min amidation reaction ti me].