Ring Closure and Ring Opening as Useful Scaffold Hopping Tools in Agrochemistry

Ring closing acyclic parts of a molecular scaffold orthe oppositemanipulation, opening rings to produce pseudo-ring structures, isan important scaffold hopping manipulation. Analogues derived frombiologically active compounds through the utilization of such strategiesare often similar in shape and physicochemical properties and, therefore,likely to exhibit similar potency. This review will demonstrate howseveral different ring closure techniques, such as replacing carboxylicfunctions by cyclic peptide mimics, incorporating double bonds intoaromatic rings, tying back ring substituents to a bicyclic structure,cyclizing adjacent ring substituents to an annulated ring, bridgingannulated ring systems to tricyclic scaffolds, and exchanging gem-dimethyl groups by cycloalkyl rings, but also ring openingled to the discovery of highly active agrochemicals.

Automated summary

Ring closing and opening manipulations of molecular scaffolds are important for scaffold hopping. Analogues derived from biologically active compounds through these strategies often show similar potency due to similar shape and physicochemical properties. This review demonstrates how various ring closure techniques, such as replacing carboxylic functions with cyclic peptide mimics, incorporating double bonds into aromatic rings, and tying back ring substituents, as well as ring opening, have led to the discovery of highly active agrochemicals.