2010-11-09

Pyrazole amides: research and development of microbicides for the next new hot spot

Pyrazole amides as Sha Junji development from the 90s of last century, Japan's Sumitomo Chemical and Mitsui Chemicals, there have been reports of relevant research and development, but after 10 years in the Sha Junji time did not cause any waves on the market. However, like the strong interest "in silence" and enter the 21st century, especially in recent years, bactericidal activity of pyrazole amide compounds in research and development as if fungicides indicates the development of another new hot spot. Pesticide giant Bayer, BASF, Syngenta and DuPont have entered this field of research and development, each of these fungicides are new varieties under development, is busy waiting to enter the market, enough attention. The new structure is characterized by chemical, broad-spectrum fungicide effective and may be different from the existing mode of action.
The earliest reported pyrazole amide fungicides are discovered and developed by Sumitomo Chemical of furosemide topiramate bacteria amine (furametpyr), test, code-named S 658 and S 82658. Alleged that the fungicides on rice sheath blight control effect of the fine, first in Japan in 1996 to obtain registration, and listed in 1997, the trade name Limber. However, the variety in the 10 years after the listing does not form between the significant market share.
Topiramate bacteria thiazolyl amine (penthiopyrad) is the second pyrazole amide fungicides, test code MTF753, Japan's Mitsui Chemicals by the discovery and development. The variety in 1999 entered a stage of development since 2000 in Japan and France began to conduct extensive field trials, and continued until 2005, and achieved satisfactory results of field trials. Its excellent rust and Sclerotinia activity, gray mold, powdery mildew, downy mildew and apple scab, also with good control effect. Mitsui Chemicals in 2007 and 2008, respectively, under the trade name applications in Japan Gaia He Affet recorded for lawn and fruit trees and vegetables, disease control, registration applications submitted to the U.S. EPA to seek in the global market development.
Mitsui Chemicals, 2007, authorized by DuPont in the Americas, Europe and Australia with market development, thiophene pyrazole amine formulations bacterial products.Year, DuPont has the European Union, the United States and Canada, trade name applications for two new fungicides Vertisan Fontelis and product registration, respectively, for a variety of fruits, vegetables, and cereal crops such as wheat, barley and soybeans, market expectations and in 2011 approved DuPont also plans to develop more bacteria containing thiophene pyrazole amine fungicides new products.
Isopyrazam, test code-named 520, was recently approved in the United Kingdom registered pyrazole amides, by the discovery and development of Syngenta. The varieties that contain a mixture of four optical isomers. Alleged that the fungicide with broad-spectrum activity against a variety of crops on the prevention and treatment of diseases with outstanding performance, the triazole and strobilurin resistant strains of bacteria and efficient, especially for shell-pin sp (Septoria) fungi is very high, such as wheat rust and rot of barley rust prevention is better than Epoxiconazole effect. The effect of fungicides to protect the main, but in the field trials also showed a therapeutic effect. With a persistence length of its features, 7 weeks after spraying showed significant results, the protection of triazole fungicides than the length of about two weeks. The company expects to establish after the listing of crop disease control and enhance the new benchmark, and fungicides to enhance and consolidate the company's market position. Isopyrazam market positioning, including fruit, vegetables and cereal crops. In the UK is about to contain isopyrazam 62.5 g / L and cyprodinil 187.5 g / L of complex products, brand name Bontima, will be used for winter barley and spring barley on disease control, and plans to enter the U.S. market in 2011.
Sedaxane is Syngenta another late in the research and development of pyrazole amide fungicides, which also contains a mixture of four optical isomers. Because it is just recently made public the details are not known, but the initial market position may be used for seed treatment.
Bixafen open in 2006, discovered and developed by Bayer. Succinate dehydrogenase inhibitor allegedly bixafen is, will be mainly developed for the control leaf spot and leaf rust and fungicide resistance management is expected to become an important species. The species listed in 2011, the company expects sales of its potential peak value over 430 million U.S. dollars.
Penflufen Bayer in the development stage is another pyrazole amide fungicides, bacteria with topiramate thiophene amine very similar chemical structure, is a typical optimization results. Currently, Bayer has submitted to the U.S. EPA registration in order to seek development in the global market will be developed for corn, cotton, rapeseed, vegetables, rice and soybeans and other crops on disease control, listed in 2012.
Recently, BASF also announced a new pyrazole amide fungicides, with the structure of Bayer's bixafen similar, with the same pyrazole benzidine structure. The compound test, code-named BAS700F, made earlier this year just ISO common name fluxapyroxad, its first product in the product name will be Xemium. In field trials, the variety of cereal crops, soybeans, corn and rape against the disease has an excellent effect, with excellent uptake and activity within. Currently, BASF is also submitted registration applications to the U.S. EPA to seek in the global market development, scheduled for 2012, promotion in the Americas and Europe.

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