The synthesis of stable isotope labeled (SIL) complex drug molecules with a ≥3 mass unit increase from the parent compound is essential for drug discovery and development. Typical approaches that rely on 2H, 13C, and 15N isotopes can be very challenging or even intractable, and can delay the drug development process. This work introduces a new concept for the synthesis of labeled compounds that relies on the use of 34S. The synthetic utility of 34S was demonstrated with the efficient synthesis of [34S]phosphorothioates [34S2]‐PS‐ODNs‐TTT and [13C, 15N, 34S]‐ceftolozane. In addition, a procedure for the direct oxidation of phosphites to [34S]phosphorothioates using elemental 34S without isotope dilution was developed.
34S: A new opportunity for the efficient synthesis of stable isotope labeled compounds
Ren, S., Fier, P. S., Ren, H., Hoover, A. J., Hesk, D., Marques, R., & Mergelsberg, I. (2018). 34S: A new opportunity for the efficient synthesis of stable isotope labeled compounds. Chemistry - A European Journal, 24(28), 7133-7136. https://doi.org/10.1002/chem.v24.28
Abstract
Publications Info
To contact an RTI author, request a report, or for additional information about publications by our experts, send us your request.
Meet the Experts
View All ExpertsRecent Publications
Article
Multifaceted risk for non-suicidal self-injury only versus suicide attempt in a population-based cohort of adults
Article
Long-term effects of a diet supplement containing Cannabis sativa oil and Boswellia serrata in dogs with osteoarthritis following physiotherapy treatments
Article
Pregnancy rates and clinical outcomes among women living with HIV enrolled in HPTN 052
Article