Comprehensive explanation of pesticides of trifluoromethylpyridine derivatives

At present, fluorinated pesticides account for about 15% of the total pesticide market. However, from 2000 to now, the share of fluorochemicals in pesticide development has increased significantly to 46%. Heterocyclic compounds are also a major focus in current market research. Pyridine rings, in particular, are common impurities found in many pesticide formulations. Among the registered pesticides, trifluoromethylpyridine derivatives are widely used, with applications including herbicides, insecticides, and fungicides. Specifically, there are 26 herbicides, 17 insecticides, and 5 fungicides based on these derivatives. Several herbicides utilize this structure. For example, five herbicides include flupirtine, pirfenoxacilin, high-efficiency pyridoxine (acid), high-efficiency pirfenoxacillin (ester), and others. These are fatty acid synthesis inhibitors, applied post-emergence in broad-leaved crop fields. They are commonly used in soybeans, peanuts, cotton, rapeseed, potatoes, watermelons, and sweet potatoes, as well as in nurseries and orchards. Their intermediate is 2,3-dichloro-5-trifluoromethylpyridine. Another group includes five herbicides such as flurazepam, flufenoxacil, fluarifop, fluazifop-P-butyl, and penoxsulam. These are acetyl-CoA carboxylase inhibitors, effective against grassy weeds without harming broad-leaved crops. They are used in soybean, cotton, potato, tobacco, flax, and vegetable fields. Their intermediate is 2-chloro-5-trifluoromethylpyridine. There are four herbicides in the fluazioxasulfuron series, including flurazine, flupyrsulfuron, flazasulfuron, and sulfoxamide. These are acetolactate synthase (ALS) inhibitors, known for their high efficiency, low dosage, and environmental safety. They are among the most popular herbicides globally due to their selectivity and low toxicity. Three other herbicides include thiabendazole, flurazepam, and flupirazin. Thiabendazole was developed by Monsanto and is used for pre-emergence weed control in fruit trees, forests, and cotton. Flunarizine is another pyridine-based herbicide, used in rice fields and lawns to control annual weeds like alfalfa and ragweed. Fluroxypyr, developed by Syngenta, is a broad-spectrum herbicide targeting various weeds. Fungicides such as oxystrobin, fluazimide, fluazinam, and fluopyram are also significant. Oxystrobin, developed by DuPont, is a mitochondrial respiratory inhibitor used for foliar diseases in wheat. It generated $0.5 billion in sales in its first year and continued to perform well, reaching $115 million in 2009. Fluopyram, developed by Bayer, targets oomycetes and is used across over 70 crops, with a strong market presence since 2011. Insecticides include chlorfluazuron, imidacloprid, sulfoxaflor, and flonicamid. Chlorfluazuron, a chitin biosynthesis inhibitor, is effective against lepidopteran pests and is considered a "green pesticide." Imidacloprid, developed by Novartis, is a neonicotinoid insecticide used widely in pest control. Sulfoxaflor, developed by Dow AgroSciences, targets aphids and planthoppers, while flonicamid has a unique mechanism that makes it highly effective against certain pests. Herbicides make up around two-thirds of this chemical class, while insecticides and fungicides account for the remaining third. Similar structures often lead to multiple products, such as the pirfenoxacilin and flupirtine series. Chlorfluazuron remains a top-selling insecticide, and flonicamid’s unique mode of action has drawn attention. Oxystrobin, as a fungicide, is widely used and economically significant. The intermediates 2,3-dichloro-5-trifluoromethylpyridine and 2-chloro-5-trifluoromethylpyridine are crucial in pesticide synthesis and hold considerable development potential.

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