Practical one-pot amidation of -Alloc-, -Boc-, and -Cbz protected amines under mild conditions.

A facile one-pot synthesis of amides from -Alloc-, -Boc-, and -Cbz-protected amines has been described. The reactions involve the use of isocyanate intermediates, which are generated in the presence of 2-chloropyridine and trifluoromethanesulfonyl anhydride, to react with Grignard reagents to produce the corresponding amides. Using this reaction protocol, a variety of -Alloc-, -Boc-, and -Cbz-protected aliphatic amines and aryl amines were efficiently converted to amides with high yields. This method is highly effective for the synthesis of amides and offers a promising approach for facile amidation.