Issue 17, 2022

Advances in solid-phase peptide synthesis in aqueous media (ASPPS)


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.

Graphical abstract: Advances in solid-phase peptide synthesis in aqueous media (ASPPS)

Article information

Article type
Critical Review
20 Jun 2022
02 Aug 2022
First published
06 Aug 2022
This article is Open Access
Creative Commons BY license

Green Chem., 2022,24, 6360-6372

Advances in solid-phase peptide synthesis in aqueous media (ASPPS)

D. M. M. Jaradat, O. Al Musaimi and F. Albericio, Green Chem., 2022, 24, 6360 DOI: 10.1039/D2GC02319A

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