ABSTRACT We explored aryl thianthrenation as a tool for directly incorporating multiple isotopes into molecular scaffolds starting from full isotopically labeled benzene. Stable isotope‐labeled (SIL) molecules are indispensable tools for investigating chemical and biological mechanisms and quantifying metabolites. However, the late‐stage incorporation of isotopically labeled benzene remains challenging and under‐investigated. This challenge stems from the direct functionalization of non‐substituted benzene, which remains a difficult task. The approach described in this work is based on sulfonium salts used as a source of 13 C 6 and 2 H 5 benzene under palladium catalysis conditions. This approach demonstrates its efficiency in C─C and C─S bond formation with different substrates. Additionally, this methodology was employed for the synthesis of poly‐substituted 13 C 6 benzene derivatives.
Labiche et al. (Tue,) studied this question.