Lopez, John, Bucher, Christoph, Beck, Janina, Berthelmann, Arne, Spyridon, Markos and Eisser, Stefan (2022) THE MISSING LINK: ENABLING LOADING OF 2-CHLOROTRITYL CHLORIDE RESIN IN N-BUTYLPYRROLIDINONE AS A GREEN SOLVENT. Organic Process Research & Development, 26 (5). pp. 1450-1457. ISSN 1083-61601520-586X

Abstract

2-Chlorotrityl chloride resin is one of the most frequently used and most versatile resins for the large-scale manufacture of peptides. As a part of our efforts in greening solid phase peptide synthesis, here we disclose an efficient procedure for the loading of the first amino acid onto 2-chlorotrityl chloride resin using the green solvent N-butylpyrrolidinone. The application of design of experiment models allowed us to identify key critical parameters in the loading process. Results obtained herein suggest that the conditions found can be generalized and applied to any Fmoc amino acid, or serve as a starting point for loading optimization.

Item Type:	Article
Keywords:	Loading of resins, DoE, Solid Phase Peptide Synthesis, SPPS,
Date Deposited:	24 Jun 2022 00:45
Last Modified:	24 Jun 2022 00:45
URI:	https://oak.novartis.com/id/eprint/44843