Piperidines and their derivatives have become increasingly popular building blocks in a vast array of synthetic protocols. The piperidine ring, a six-membered ring containing one nitrogen atom, can be recognized not only in the structure of more than half of the alkaloids known today, but also in many natural or synthetic compounds with interesting biological activities. 1-Boc-2-(aminomethyl)piperidine has been used in a post-Ugi carbonylation/intramolecular amidation approach to a series of eight-membered macrolactams with multiple points of diversity.