3920935

Mesoionic Pyrido[1,2-α]pyrimidinones as Insecticides

Date
August 16, 2023
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The rising global population creates a critical need to ensure a robust and reliable food supply. As such, the prevention of insect damage to crops is of significant importance to both farmers and consumers. This creates a necessity to discover insecticides with novel modes-of-action, as insect species are continuously evolving to become resistant against current and existing active ingredients.
A novel class of mesoionic pyrido[1,2-a]pyrimidinones, such as compound I, was serendipitously discovered as a side product during a fungicidal optimization program. Compound I exhibited weak activity in our laboratory insecticidal screens. The optimization of mesoionic I for its insecticidal properties resulted in the discovery of two novel insecticides with interesting spectrum: Triflumezopyrim controls delphacid and cicadellid hoppers and Dicloromezotiaz controls a broad range of lepidoptera. We will report the optimization program that led to the discovery of Triflumezopyrim and Dicloromezotiaz. Our efforts in the rational design, synthesis, and structure-activity relationships will be presented.

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