Advances in solid-phase peptide synthesis in aqueous media (ASPPS). Issue 17 (15th August 2022)

• Record Type: Journal Article
• Authors: Jaradat, Da'san M. M.; Al Musaimi, Othman; Albericio, Fernando
• Is Part Of: Green chemistry. Volume 24:Issue 17(2022)
• Page Start: 6360
• Page End: 6372
• Publication Date: 2022-08-15
• Subjects: Environmental chemistry -- Industrial applications -- Periodicals; Environmental management -- Periodicals; 660
• DOI: 10.1039/d2gc02319a
• Languages: English
• ISSNs: 1463-9262

Abstract

Abstract : Technologies to enable Aqueous Solid-Phase Peptide Synthesis (ASPPS). Abstract : Peptides have been gaining ground in the pharmaceutical arena, with a total of 22 approvals over the last six years. These molecules are also present in antibody–drug conjugate constructs as linkers or payloads, or both. Solid-phase peptide synthesis (SPPS) is the method of choice for peptide synthesis. The introduction of an automatic synthesizer facilitated this methodology and helped in reducing the amounts of the required solvents. However, there are still concerns regarding the amounts, as well as the safety profiles, of the solvents involved in SPPS. Here, we discuss the work addressing the use of water as the greenest alternative to the common non-green solvents employed in various steps of the SPPS methodology. Various technologies were introduced which enabled the synthesis of di- and up to decapeptides in aqueous media with satisfactory yields and purities.