A groundbreaking advancement in chemical synthesis has been achieved by a Chinese research team, led by Zhang Xiaheng from the Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences. Their innovative method, recently published in the prestigious journal Nature, revolutionizes the application of aromatic amines, offering a safer and more efficient alternative to traditional industrial processes. Aromatic amines, essential components in pharmaceuticals, agrochemicals, and natural products, have long been underutilized due to the inherent risks and inefficiencies of conventional methods. For over a century, industries have relied on converting aromatic amines into diazonium salts, which are highly explosive and unstable. This process also suffers from excessive copper reagent consumption and limited substrate compatibility. To overcome these challenges, the team dedicated three years to developing a novel direct deaminative functionalization technology. This method utilizes common and inexpensive laboratory reagents, enabling the efficient conversion of inert aromatic carbon-nitrogen bonds into various crucial chemical bonds. The new approach is highly versatile, applicable to nearly all types of medicinal heteroaromatic amines and aniline derivatives, regardless of their electronic properties or amino group positions. It also supports kilogram-scale production through straightforward operations. Zhang emphasized that this breakthrough opens new pathways for rapidly constructing complex molecules from readily available starting materials, significantly advancing research and development in medicinal chemistry.