To demonstrate the efficiency of our protocol, amide 1 was prepared on a 100 mmol scale (Scheme 3), using the solid-phase work-up procedure to purify the amide. This gave 21.23 g of amide 1 in 97% overall yield. The process mass intensity for the reaction was calculated to be 8, showing that this catalytic amidation method is extremely competitive for use in large scale preparations (e.g. a typical PMI for stoichiometric amidation reactions used in the synthesis of pharmaceutical intermediates is ~43 6 ).