Both couplings and deprotections for solution- and solid-phase peptide synthesis can be carried out in the polar aprotic solvent propylene carbonate.

The use of a range of green solvents to swell a diverse range of resins used in solid-phase synthesis is investigated.

No abstract

Solid-phase organic synthesis is an essential method for the rapid synthesis of complex biological structures and libraries of small organic molecules. However, it is often associated with the use of large quantities of problematic solvents for the removal of excess reagents and reaction by-products. Given that solvent will often be the biggest contributor to waste generated in the average pharmaceutical/fine-chemical process, its exchange for a more desirable alternative often presents the biggest gains in terms of reducing environmental impact. This review aims to explore recent approaches to performing solid-phase organic synthesis, and associated solid-phase peptide synthesis, in neoteric solvents and reaction media that present greener alternatives.

Polymer–drug conjugates have received considerable attention over the last decades due to their potential for improving the clinical outcomes for a range of diseases. It is of importance to develop methods for their preparation that have simple synthesis and purification requirements but maintain high therapeutic efficacy and utilize macromolecules that can be cleared via natural excretory pathways upon breakdown. Herein, the combination of ring‐opening polymerization (ROP) and reversible addition−fragmentation chain‐transfer (RAFT) polymerization is described for the straightforward synthesis of amphiphilic, stimuli‐responsive, biodegradable, and highly functionalizable hyperbranched polymers. These unimolecular nanoparticles demonstrate a versatile platform for the synthesis of polymer–drug conjugates owing to the inclusion of a Boc‐protected polycarbonate moiety in either a block or random copolymer formation. A proof‐of‐concept study on the complexation of the poorly water‐soluble antimicrobial drug usnic acid results in polymer‐drug complexes with powerful antimicrobial properties against gram‐positive bacteria. Therefore, this work highlights the potential of amphiphilic and biodegradable hyperbranched polymers for antimicrobial applications.