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The University of Chinese Academy of Sciences announced that recently, the team led by Zhang Xiaheng, a researcher at the Hangzhou Advanced Institute of the University of Chinese Academy of Sciences, published new research findings in the journal Nature. They proposed a novel method that utilizes N-nitramine to achieve direct deamination and functionalization, thereby overturning the traditional processes that have been used in the industrial sector for 140 years. Aromatic amines are one of the extremely common functional groups among bioactive molecules. Over the past century or so, in the industrial sector, aromatic amines have typically been first converted into intermediates known as \"diazonium salts,\" and subsequent transformations are then carried out taking advantage of the high reactivity of these diazonium compounds. This stepwise strategy has numerous drawbacks, such as the poor stability of diazonium salts and their explosive nature; processes based on aryl diazonium salts also face issues including high consumption of copper in stoichiometric amounts and limited substrate compatibility. To overcome these challenges, Zhang Xiaheng’s team spent three years working diligently to find a direct activation pathway for aromatic amines. Ultimately, the team successfully developed a new direct deamination functionalization technique using common and inexpensive chemical reagents available in laboratories. This study utilizes aromatic amines to form N-nitramine intermediates in situ under nitric acid mediation, and subsequently achieves an efficient direct conversion of aromatic carbon-nitrogen bonds into various C-X bonds (including carbon-halogen bonds, carbon-oxygen bonds, carbon-nitrogen bonds, and carbon-carbon bonds) as well as carbon-carbon bonds, through the removal of dinitrogen monoxide. To further improve operational convenience, the research team also developed a one-pot deamination cross-coupling strategy. By simply adding the appropriate coupling reagents directly to the deamination reaction intermediates, multiple cross-coupling reactions can be carried out in the same reaction system. This approach utilizes only common reagents available in laboratories, enabling the efficient large-scale production of target products in kilogram quantities. It holds the potential to improve the traditional processes that have been in use in the industrial sector for 140 years, offering a safe and cost-effective alternative to aryl diazonium chemistry, which is currently limited due to its explosiveness and high risks. This method can find wide application in various important fields such as pharmaceuticals and material manufacturing. It is reported that this achievement was highly praised by the four chief reviewers at the journal Nature. Scott Bagley, Senior Director of Research and Development at Pfizer, one of the international pharmaceutical giants serving as a reviewer, described it as a “true tour de force” (French: a genuine masterpiece).