Chinese scientists develop breakthrough method for aromatic amine applications

BEIJING -- A Chinese research team has developed an advanced method to overcome long-standing challenges in the application of aromatic amines, promising a safer and more efficient alternative to an old industrial process, according to a study recently published in the journal Nature.

The research, led by Zhang Xiaheng from the Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, introduces a novel strategy that efficiently converts inert aromatic carbon-nitrogen bonds into various crucial chemical bonds.

Aromatic amines are fundamental structural components widely found in pharmaceuticals, agrochemicals and natural products. However, their potential as versatile building blocks in synthesis has remained underdeveloped.

For over a century, industrial practices have relied on converting aromatic amines into diazonium salts -- intermediates known for their high explosiveness and instability. This conventional approach suffers from significant drawbacks, including safety hazards, excessive copper reagent consumption, and limited substrate compatibility.

To address these challenges, the research team spent three years dedicated to exploring direct activation pathways for aromatic amines. Ultimately, they successfully developed a novel direct deaminative functionalization technology using common and inexpensive laboratory reagents.

The new method offers significant advantages for poly-nitrogen heterocyclic systems commonly used in drug synthesis. With simple and readily available laboratory reagents, it exhibits excellent versatility -- applicable to almost all types of medicinal heteroaromatic amines and aniline derivatives with diverse electronic properties and structures, regardless of amino group position. Moreover, it enables kilogram-scale production through straightforward operations.

This research opens up a new pathway for rapidly constructing complex molecules from readily available starting materials, offering significant potential for advancing research and development in medicinal chemistry, Zhang said