Lopez, John, Albericio, Fernando, de la Torre, Beatriz and Ramkisson, Shaveer (2021) Refractive Index: The Ultimate Tool for Real-Time Monitoring of Solid-Phase Peptide Synthesis. Greening the Process. Organic process research & development, 25. pp. 1047-1053. ISSN 1520-586X; 1083-6160

Abstract

This is the OAK Entry for the series of conferences where the content of OAK case 44094 (previously approved) is presented.

Peptides are the basis of many drugs currently in the market and much more entering clinical trials, as well as in preclinical studies. The most part of peptides in both research and industrial modes are synthesized using Solid-Phase Peptide Synthesis (SPPS) processes. A characteristic of this strategy is that the synthetic intermediates are not isolated and not characterized. In this context, the development of a real-time monitoring method would assure an optimal synthetic process. Refractive index (RI) of a liquid has important information about its physical properties and makes it possible to know the composition of any solution. Herein, RI is demonstrated for the first time as a Process Analytical Tool (PAT) that can be used for real-time monitoring of SPPS. The three basic steps involved in this process can be followed up on line: coupling, deprotection and washes. This has consequences for the determination of the end-point of the reactions and the optimization of all synthetic steps. This will impact directly into the consumption of reagents, solvents, and time, making SPPS greener.

Item Type:	Article
Date Deposited:	24 Jun 2022 00:45
Last Modified:	24 Jun 2022 00:45
URI:	https://oak.novartis.com/id/eprint/45071