Peptides as drugs show unique characteristics (high biological activity, high specificity and low toxicity), thereby making them particularly attractive therapeutic agents. During the last years, the pharmaceutical industry, which was traditionally focused on small molecules, has been attracted by the benefits that peptides confer. This is due in part, for the great number of developments carried out in their synthetic strategies, mostly in the Solid-Phase mode.

Solid-Phase Peptide Synthesis is based in a proper combination of several parameters: the solid support, the handle which links the growing peptide to the solid support, the protecting groups, and the coupling method. Herein, the recent strategies developed by our group will be discussed. These involve the use of ChemMatrix resin for the preparation of libraries, a free side-reaction Wang linker, the backbone N-(4-azidobutyl) linker for peptide conjugation, Phacm, Dpm, S-TMP, and Cys-pseudoproline for the Cys protection, NCS for disulfide formation, KOxyma as coupling additive, and BOP-OXy, BOP-OBt, and BOP-AOt as coupling reagents.