Efficient Synthesis of Ractopamine‐D₃ via Epoxide‐Opening Strategy

Abstract

The incorporation of deuterium isotopes into illicit additives like ractopamine holds significant promise for enabling swift and accurate detection. However, current synthetic methodologies for deuterium labeling often involve intricate and time‐consuming processes, necessitating laborious de/protection steps and specialized equipment. Herein, after establishing efficient epoxide‐opening reactions using diverse primary amines, a practical, efficient and straightforward synthetic route for producing deuterium‐labeled ractopamine‐D3 has been successfully established, which was confirmed by 1H‐NMR and ESI‐MS with a deuterium isotope abundance exceeding 98 atom% D. Remarkably, this newly devised convergent synthetic protocol, encompassing just three steps, delivered up to 53% overall yield of ractopamine‐D3, underscoring its scalability and potential pharmaceutical viability.