The tea-bag protocol for comparison of Fmoc removal reagents in solid-phase peptide synthesis

• DOI: 10.1007/s00726-020-02883-8
• Publication Date: 2020-08-26T18:03:54Z
• Authors: Fanny Guzmán; Adriana Gauna; Omar Luna; Tanya Román; Claudio Álvarez; Fernando Albericio; Constanza Cárdenas
• Keywords: Piperidine; Piperazine; Peptide Synthesis

Several factors have influenced the increasing presence of peptides as an important class of Active Pharmaceutical Ingredients. One is the continued development of synthetic methodologies for peptide synthesis. Herein, we investigated the Fmoc removal step, using the tea-bag strategy. In this regard, three different secondary amines: piperidine, 4-methylpiperidine, and piperazine, were evaluated. As a result of this study, 4-methyl piperidine showed to be an excellent alternative to the usually used piperidine in terms of purity and compliance with green chemistry principles as well.