Optimized Stepwise Synthesis of the API Liraglutide Using BAL Resin and Pseudoprolines release_stkp7txhgnbfbbwygj23gfby5e

by Daniel Carbajo, Ayman El-Faham, Miriam Royo, Fernando Albericio

Published in ACS Omega by American Chemical Society (ACS).

2019   Volume 4, Issue 5, p8674-8680

Abstract

The number of peptide-based active pharmaceutical ingredients (APIs) has increased enormously in recent years. Furthermore, the emerging new peptide drug candidates are more complex and larger. For the industrial solid-phase synthesis of C-carboxylic acid peptides, the two main resins available, Wang and chlorotrityl chloride (CTC), have a number of drawbacks. In this context, resins that form an amide bond with the first amino acid are more robust than Wang and CTC resins. Here, we address the use of the backbone (BAL) resin for the synthesis of the peptide liraglutide. The BAL resin, in conjunction with the use of pseudoprolines to avoid aggregation, allows the stepwise solid-phase synthesis of this API in excellent purity and yield.
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