Wu, XuanYao, YaoWang, LianhongZhou, DashunSun, FeifeiChen, JianqiuJi, RongCorvini, Philippe2022-10-042022-10-042022-03-082190-47072190-471510.1186/s12302-022-00598-zhttps://irf.fhnw.ch/handle/11654/33897https://doi.org/10.26041/fhnw-4302Background Due to their widespread use, sulfonamide antibiotics (SAs) have become ubiquitous environmental contaminants and thus a cause of public concern. However, a complete understanding of the behavior of these pollutants in complex environmental systems has been hampered by the unavailability and high cost of isotopically labeled SAs. Results Using commercially available uniformly [14C]- and [13C]-labeled aniline as starting materials, we synthesized [phenyl-ring-14C]- and [phenyl-ring-13C]-labeled sulfamethoxazole (SMX), sulfamonomethoxine (SMM), and sulfadiazine (SDZ) in four-step (via the condensation of labeled N-acetylsulfanilyl chloride and aminoheterocycles) or five-step (via the condensation of labeled N-acetylsulfonamide and chloroheterocycles) reactions, with good yields (5.0–22.5% and 28.1–54.1% for [14C]- and [13C]-labeled SAs, respectively) and high purities (> 98.0%). Conclusion The synthesis of [14C]-labeled SAs in milligram amounts enables the preparation of labeled SAs with high specific radioactivity. The efficient and feasible methods described herein can be applied to the production of a variety of [14C]- or [13C]-labeled SAs for studies on their environmental behavior, including the fate, transformation, and bioaccumulation of these antibiotics in soils and aqueous systems.en600 - Technik, Medizin, angewandte Wissenschaften01A - Beitrag in wissenschaftlicher Zeitschrift