A retrospective look at anthranilic diamide insecticides: discovery and lead optimization to chlorantraniliprole and cyantraniliprole

TLDR

Anthranilic diamides are a key class of insecticides that selectively target insect ryanodine receptors, with chlorantraniliprole showing strong lepidopteran activity and cyantraniliprole offering broad‑spectrum efficacy across lepidopteran and hemipteran pests. The study retrospectively examines the discovery of anthranilic diamides and the chemistry that led to chlorantraniliprole and cyantraniliprole. It traces the lead‑optimization process that evolved the initial compounds into the two commercial products. © 2016 Society of Chemical Industry.

Abstract

Anthranilic diamides are an important commercial synthetic class of insecticides (IRAC Group 28) that bind to the ryanodine receptor with selective potency against insect versus mammalian forms of the receptor. The first commercialized diamide, chlorantraniliprole, has exceptional activity against lepidopteran pests. The second anthranilamide product, cyantraniliprole, has excellent cross-spectrum activity against a range of insect orders, including both lepidopteran and hemipteran pests. Here, a retrospective look is presented on the discovery of the class, along with chemistry highlights of the lead evolution to both products. © 2016 Society of Chemical Industry.