A Reusable Polystyrene Support for Sustainable yet Cost-effective Octreotide Synthesis

The synthesis of peptide drugs has become facile with the use of supports that enable easy separation of the growing peptide. Peptide synthesis on insoluble supports typically employs excess reagents to enhance reaction efficiency and faces challenges during intramolecular cyclization. A non-crosslinked soluble polystyrene support is reported herein that improves cyclization efficiency on the support by using spacers. The support efficiency is illustrated by synthesizing octreotide drug in a scalable manner by on-support cyclization. The methodology drastically reduces the reagent waste, raw-material cost, and solvent requirement. The support can also be recovered and re-used up to 3 times making this a very sustainable method.