“直接脱氨”策略有望降低药物成本

Core Viewpoint - The research team led by Zhang Xiaoheng from the University of Chinese Academy of Sciences has developed a new method for modifying aromatic amines, which could significantly reduce costs in cancer drug production and eliminate risks associated with traditional methods [2][5]. Group 1: Research Breakthrough - The team published their findings in "Nature," highlighting a novel "direct deamination" strategy that replaces stable carbon-nitrogen bonds in aromatic amines with various functional chemical bonds using inexpensive reagents [2][5]. - This new method avoids the use of unstable diazonium salt intermediates, which pose explosion risks and contribute to heavy metal pollution [4][5]. Group 2: Industrial Implications - The traditional method for removing amino groups from aromatic amines has been in use for over 140 years, but it is inefficient and environmentally unfriendly, leading to high costs in drug production [3][4]. - The new approach is expected to lower the production costs of certain drug intermediates by 40%-50% and facilitate large-scale green production [8]. Group 3: Methodology and Process - The research involved extensive experimentation, leading to the discovery that N-nitrosoamines, initially considered a minor byproduct, play a crucial role in mediating the synthesis of target products [6][7]. - The team developed a one-pot deamination cross-coupling strategy, allowing multiple reactions to occur within the same system, enhancing operational convenience [7]. Group 4: Future Prospects - The new method has been tested on various nitrogen-containing intermediates commonly used in the pharmaceutical industry, showing applicability across different types of drug precursors [8]. - While initial laboratory-scale validations have been completed, further research and industrial testing are required to fully realize the method's potential and ensure safety in larger-scale applications [9].