Abstract

Aryloxy phenoxy propionic acid esters (APP) chiral herbicide is a kind of acetyl coenzyme A carboxylase enzyme (Acetyl CoA Carboxylase) inhibitor. Sulfonylureas and diphenylethers herbicide are the acetohydroxyacid synthase (ALS) inhibitors and 4,6-dimethoxypyrimidine is the major active group. Bioisosterism and active group combination principle were the primary and effective ways to develop novel pesticides. By using the above principles, we synthesized phenoxy propionate and phenoxy acetamide compounds which containing 4,6-dimethoxypyrimidine. Bioassay results showed that these compounds have no obvious herbicidal activities, but some of them showed higher inhibitory activities for cucumber downy mildew (Pseudoperonospora cubensis) and tomato late blight (Phytophthora infestans), the individual compounds showed milder inhibitory activities for wheat powdery mildew (Blumeria graminis) and rice blast (Pyricularia grisea).

Keywords: Synthesis, bioactivity, 4, 6-dimethoxypyrimidine, phenoxy carboxylate, fungicidal activity.

Graphical Abstract