新方法颠覆140年制药工艺

Core Insights - 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 impact the pharmaceutical industry by reducing costs and improving safety in drug synthesis [1][2][3] Group 1: Research Breakthrough - The team introduced a "direct deamination" strategy that replaces stable carbon-nitrogen bonds in aromatic amines with various functional chemical bonds, avoiding the use of hazardous diazonium intermediates [1][3] - This new method is expected to address the cost challenges associated with anticancer drugs and has received high praise from industry experts, including Pfizer's senior R&D director [1][2] Group 2: Traditional Method Limitations - The traditional method for removing amino groups from aromatic amines involves converting them into unstable diazonium salts, which pose explosion risks and generate significant waste [2][4] - The existing process is not aligned with current green chemistry goals, as it consumes large amounts of copper and incurs high pollution treatment costs [2][4] Group 3: Innovative Approach - The research involved extensive experimentation, leading to the discovery that N-nitrosoamines, initially considered a minor byproduct, play a crucial role in facilitating the synthesis of target products [4][5] - The new method allows for the direct cleavage of carbon-nitrogen bonds under mild conditions, using inexpensive reagents, and eliminates the need for hazardous intermediates [5][6] Group 4: Industrial Application Potential - The new strategy has been tested on various nitrogen-containing intermediates commonly used in pharmaceuticals, demonstrating its applicability across a wide range of drug precursors [6] - Collaborations with pharmaceutical companies are underway to implement this technology in the synthesis of drug intermediates, potentially reducing production costs by 40%-50% [6]