The continuing significance of chiral agrochemicals

Abstract

Chemical crop protection is one of the most cost-effective methods for agriculture, as crop failures can be prevented, and sustainable growth can be enabled regardless of the seasons. Agricultural production must be significantly increased in the future to meet the food needs of a growing world population. However, the continued loss of established active ingredients due to consumer perceptions, changing needs of farmers and ever-changing regulatory requirements is higher than annually new active ingredients introduced to the market. The development of innovative active ingredients is therefore essential to continuously improve the selectivity, efficacy and favorable environmental profile of agrochemicals. Molecules with stereogenic centers can be considered here, as they often have different properties than non-chiral molecules. Natural products and their congeners are still a valuable source of inspiration for chiral agrochemicals. However, only a few novel chiral agrochemicals are currently produced on an industrial scale as pure stereoisomers or in enriched form. As of 2018, around 43% of the 35 chiral products introduced to the market (herbicides, fungicides, insecticides, acaricides, and nematicides) contain one or more stereogenic centers in the molecule, and almost 69% of them have been marketed as racemic mixtures of enantiomers or stereoisomers. Surprisingly, the proportion of chiral agrochemicals is in the same order of magnitude as in the time frame from 2007 to 2017 with around 42%, respectively. This report therefore provides an overview of the continued importance of chiral agrochemicals brought to market in the last 6 years and describes the inherent related challenges of modern agrochemicals through the management of key aspects arising from innovative crop protection products. © 2025 The Author(s). Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.