Chapter 13 2,4-Diaminoquinazoline Insecticides

摘要

2,4-Diaminoquinazolines are a new class of lepidopteran insecticide that perform very well in an artificial diet assay, but perform less well when the compounds are applied foliarly. 2,4-Diaminoquinazolines are readily prepared and optimized to high activity against tobacco budworm larvae in an artificial diet assay. 2,4-Dichloroquinazoline was treated with an appropriately protected 4-aminopiperidine, followed by reaction with an aniline at high temperature to prepare the desired targets. These compounds are 10 to 100-fold less active than expected in foliar assays of tobacco budworm and other lepidoptera. A number of possible reasons for this poor diet to foliar translation are explored including metabolism, physical properties and formulations.