met the requirements for use in preclinical can-
didate selection studies. We anticipate that
facile access to highly deuterated and tritiated
compounds based on the method described herein
will enable accelerated and broader interroga-
tion of the biological activity of molecules in
the pursuit of the development of new molec-
REFERENCES AND NOTES
1. E. M. Isin, C. S. Elmore, G. N. Nilsson, R. A. Thompson,
L. Weidolf, Chem. Res. Toxicol. 25, 532–542 (2012).
2. W. J. S. Lockley, A. McEwen, R. Cooke, J. Labelled Comp.
Radiopharm. 55, 235–257 (2012).
3. R. Voges, J. R. Heys, T. Moenius, Preparation of
Compounds Labeled with Tritium and Carbon-14 (John Wiley &
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1186 1 DECEMBER 2017 • VOL 358 ISSUE 6367 sciencemag.org SCIENCE
Fig. 4. Scope of high-specific-activity tritiation. Reaction conditions: substrate (2 mmol), photoredox catalyst 1 or 12 (4 mol %), thiol catalyst 13 or 14
(60 mol %), T2O (preformed from 1 Ci T2 and PtO2), NMP, rt, 34-W blue LED or
integrated photoreactor. ‡Incorporation depicted is for the 2 Ci reaction with [3H]22.