Over one billion people worldwide are infected with neglected diseases, primarily impacting low-income populations. The Distributed Drug Discovery (D3) program creates solid phase peptide synthesis (SPPS) procedures for undergraduate second semester organic chemistry courses that synthesize non-natural dipeptides to be screened for activity against pathogens causing neglected diseases. Institutions around the world participate, speeding up the drug discovery process and promoting social responsibility in young scientists. D3’s vision of socially responsible chemistry aligns well with the practice of green chemistry, which prioritizes sustainability and safety. Traditionally, SPPS uses hazardous and hard-to-access reagents and solvents, such as explosive hydroxybenzotriazole (HOBt) and toxic dimethylformamide (DMF). This study optimizes conditions using propylphosphonic anhydride (T3P) as a green coupling reagent and greener solvents, such as 2-methyltetrahydrofuran (2-MeTHF) and ethyl acetate (EtOAc). This new protocol is less expensive than the original, uses safer solvents and more accessible reagents, and is effective across a wide variety of compounds.

Using propylphosphonic anhydride (T3P) to achieve a green, accessible protocol for distributed drug discovery (D3)

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.