Tag: Mikrowelle

Professor Fernando Albericio

University of Barcelona,

University of Kwazulu-Natal

Fernando Albericio,^1,2 Beatriz G. de la Torre¹

¹University of KwaZulu-Natal, Durban 4001, South Africa; ²University of Barcelona, 08028-Barcelona, Spain

During the last five years (2016-2020), 18 drugs containing peptides have been approved by the US FDA.  In addition, several hundred are in clinical phases or advanced preclinical studies.   The development of new synthetic strategies has facilitated this explosion in the world of peptides. In this regard, the development of new resins, coupling reagents, protecting groups, and, more importantly, reliable and robust peptide synthesizers have been vital for the consolidation of the peptide drug market. 

In the field of automatic synthesizers, the last breakthrough occurred when at the beginning of this century, CEM launched the new concept of Microwave-Assisted SPPS. Our group and others have demonstrated that both couplings and Fmoc-removal are better performed in the microwave mode compared with classical synthesis or even with conventional heating. More important, this better performance in the two key reactions is not accompanied by any significant side-reaction. 

This presentation will discuss our last results on the use of Microwave synthesis for the preparation of intriguing peptides and/or for developing new synthetic strategies: (i) the preparation of staple peptides via late-stage C(sp2)-H Pd activation using the microwave; (ii) synthesis of N-alkyl amino acid containing peptides; (iii) development of new and more efficient coupling reagents; and (iv) microwave-based Green Solid-Phase Peptide Synthesis (GSPPS). 

In the GSPPS, the CEM Liberty Blue Microwave technology by itself could be considered green in terms of solvent consumption and time-saving and due to the excellent quality of the crude peptides, which enormously facilitates the purification with the consequent increase of yield and reduction of chromatography solvents.