化学“搭积木”方法

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“搭积木”法可高效构建更大分子
Ke Ji Ri Bao· 2025-06-09 23:43
Core Insights - A new chemical "building block" method developed by a team from the University of Cambridge allows for the efficient addition of single carbon atoms to molecular structures, facilitating the construction of larger molecules. This breakthrough offers a simple, universal, and scalable molecular building strategy, significantly benefiting drug development and complex chemical design [1] Group 1: Methodology and Innovation - The method focuses on a new strategy for "one-carbon-at-a-time" extension of molecular chains, specifically targeting alkenes, which are common organic compounds containing carbon-carbon double bonds. These structures are prevalent in various everyday products, including antimalarial drugs like quinine, agricultural chemicals, and fragrances [1] - Traditional methods for adding carbon atoms to molecules often require multiple reaction steps, making the process cumbersome and inefficient. The new method employs a "one-pot" chemical reaction process that greatly simplifies operational steps and enhances applicability [1] - A key component of this method is a "single carbon transfer reagent" based on allyl sulfone, designed to precisely insert a carbon atom during the reaction. This reagent first binds with the target molecule to initiate the connection reaction, then undergoes structural changes to complete the carbon addition in situ, resembling a building block assembly process [1] Group 2: Applications and Implications - To validate the method's effectiveness, the team applied it to modify the structure of the well-known immunosuppressant cyclosporin A. They successfully added one to two carbon atoms to its molecular structure, creating multiple new derivatives. Some of these new drug versions retained their immunosuppressive activity, while others lost this function, indicating that minor structural changes can significantly impact drug mechanisms, providing new possibilities for modulating drug efficacy [2] - The ability to finely adjust molecular structures is expected to drive significant advancements in medicinal chemistry, as even slight differences in molecular structure can lead to substantial variations in efficacy, toxicity, or metabolic characteristics. Additionally, the method allows for the introduction of various functional groups, further expanding the scope of molecular design [2] - Beyond pharmaceuticals, this technology has broad applications in agricultural chemicals, materials science, and other industries, particularly in scenarios requiring fine-tuning of performance through carbon chain structure adjustments [2]