Jeschke Peter
Institute of Organic Chemistry and Macromolecular Chemistry, Heinrich Heine University Düsseldorf, University Street 1, D-40225, Duesseldorf, Germany.
ChemSusChem. 2025 Jan 14;18(2):e202401042. doi: 10.1002/cssc.202401042. Epub 2024 Oct 7.
Today, the agrochemical industry faces enormous challenges to ensure the sustainable supply of high-quality food, efficient water use, low environmental impact, and the growing world population. The shortage of agrochemicals due to consumer perception, changing needs of farmers and ever-changing regulatory requirements is higher than the number of active ingredients that are placed on the market. The introduction of halogen atoms into an active ingredient molecule offers the opportunity to optimize its physico-chemical properties such as molecular lipophilicity. As early as 2010, around four-fifths of modern agrochemicals on the market contained halogen atoms. In addition, it becomes clear that modern agrochemicals have increasingly complex molecular structures with one or more stereogenic centers in the molecule. Today, almost half of modern agrochemicals are chiral molecules (herbicides, insecticides/acaricides/nematicides ≪ fungicides) and most of them consist of mixtures such as racemic mixtures of enantiomers, followed by mixtures of diastereomers and mixtures of pure enantiomers. Therefore, it is important that halogen-containing substituents or stereogenic centers are considered in the structural optimization of the active ingredients to ultimately develop sustainable agrochemicals in terms of efficacy, ecotoxicology, ease of use and cost-effectiveness.
如今，农用化学品行业面临着巨大挑战，要确保高质量食品的可持续供应、高效用水、低环境影响以及不断增长的世界人口需求。由于消费者认知、农民需求变化以及监管要求不断变化，农用化学品的短缺情况比投放市场的活性成分数量更为严重。将卤素原子引入活性成分分子中，为优化其物理化学性质（如分子亲脂性）提供了机会。早在2010年，市场上约五分之四的现代农用化学品都含有卤素原子。此外，很明显现代农用化学品的分子结构越来越复杂，分子中含有一个或多个立体中心。如今，几乎一半的现代农用化学品是手性分子（除草剂、杀虫剂/杀螨剂/杀线虫剂≪杀菌剂），其中大多数由对映体的外消旋混合物等混合物组成，其次是非对映体混合物和纯对映体混合物。因此，在活性成分的结构优化中考虑含卤素取代基或立体中心非常重要，以便最终在功效、生态毒理学、易用性和成本效益方面开发出可持续的农用化学品。
