Synthesis Principle and Practice with Radioactive Iodines and Astatine: Advances Made So Far

Abstract

Radioactive iodines and astatine, possessing distinct exploitable nuclear properties, play indispensable roles in the realms of nuclear imaging and therapy. Their analogous chemical characteristics shape the design, preparation, and substrate range for tracers labeled with these radiohalogens through interconnected radiosynthetic chemistry. This perspective systematically explores the labeling methods by types of halogenating reagents─nucleophilic and electrophilic─underpinning the rational design of such compounds. It delves into the rapidly evolving synthetic strategies and reactions in radioiodination and radioastatination over the past decade, comparing their intrinsic relationships and highlighting variations. This comparative analysis illuminates potential radiosynthetic methods for exploration. Moreover, stability concerns related to compounds labeled with radioactive iodines and astatine are addressed, offering valuable insights for radiochemists and physicians alike.