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Author: Zuo Jun
Market Manager & editor of agropages
Email: zorro@agropages.com,
Wechat: Michael Zorro, welcome to communicate!
In the 1990s, 4-hydroxyphenylpyruvate dioxygenase (HPPD) was first identified as a herbicide target. At present, HPPD has become one of the most important herbicide targets. Among more than 20 types of herbicides in the world, HPPD inhibitor herbicides, with its multiple advantages of high activity, broad killing spectrum, diverse chemical structure, continuous listing of new products, good crop safety, and no interactive resistance with existing herbicides, have maintained stable growth and rapid growth in recent years, attracted the attention of the industry and become the key herbicide varieties launched by major companies.
During 2015-2019, a total of 10 new herbicide varieties were disclosed, including 5 new HPPD inhibitor varieties: - cypyrafluone and bipyrazone, new HPPD inhibitor herbicides developed by Qingyuan nongguan, were listed in China in 2018- Fenpyrazone and tripyrasulfone, a new HPPD inhibitor herbicide developed by nongguan, Qingyuan, was approved and registered in China in January 2020, and is expected to be available in spring 2020; lancotrione, a new HPPD inhibitor herbicide developed by Shiyuan Industry Co., Ltd., Japan. At present, there are two or three candidate compounds in the later development stage (such as f9960 of FMC, fenquinotrione of Japanese combinatorial chemistry). It is predicted that these compounds will also maintain a high-speed growth trend in the next few years, with an annual growth rate of more than 10%. With the continuous development and marketing of herbicide varieties of these inhibitors, more than 10 varieties currently on the market mainly include three ketones (nitsulfuronone, cyclosulfone, dicyclosulfuronone, furasulfuronone, sulfonone, flupyrazone), pyrazoles (benzoxazolone, pyrazolone, pyrazolone, benazole, tolpyralate), Isoxazoles (isoxazolone) 。 After more than ten years of development, the market of isoxazolone has also become mature, especially in corn weeding, which has long occupied the second place in the market of herbicides and HPPD inhibitors in corn field (only next to nitrosulfosalkone), with sales exceeding 200 million US dollars in 2016, accounting for 16.5% of the market of such herbicides. Its market has grown rapidly in recent years, which is mainly due to its combination with new products and increased use in sugarcane. At present, a large number of pharmacodynamic tests have been carried out on isoxazolone in China, which provides a market-oriented basis for the promotion and application of this product in China. Discovery and development of isoxazolone
Isoxaflutole, chemical name: 5-cyclopropyl-4 - (2-methylsulfonyl-4-trifluoromethyl) benzoyl isoxazole, trade name: balance (Bayer) and Merlin (Bayer, certis Europe), etc., are HPPD inhibitor herbicides discovered by Ronald Planck company in 1992, and are now produced and sold by Bayer crop science company. According to the structure, isoxazolone belongs to isoxazole herbicide, which has broad-spectrum herbicidal activity and can control more than 50 kinds of grass weeds and broad-leaved weeds. At present, it is mainly used to control broad-leaved weeds and gramineous weeds in corn and sugarcane fields. It can be used before and after seedling. In 1996, isoxazolone was first developed in Jamaica under the trade name Merlin. In the same year, the product was registered in other Caribbean countries and some South American countries. Single agent products include balance pro (SC, 480g A.I. / L), Merlin, Provence (WG, 75g A.I. / kg), etc. The compounded products include Atoll (SC, isodiazole 37.5 + atrazine 500g a.i/l), Lagon, Merlin combi (SC, isodiazole 75 + benzophenone 500g A.I. / L), Merlin Duo (SC, isodiazole 37.5 + terbutazone 375g A.I. / L), Merlin extra / mix (SC, isodiazole 50 + atrazine 500g A.I. / L), radius (isodiazole 51.5 + fluthiazolamide 528.5g a. I. / L) and epic, Merlin GP, boreal (WG, isodiazole 100 + fluthiazolamide 480g A.I. / kg). In the United States, isoxazolone has grown strongly since it was launched and has become a best-selling product in many major corn markets. In recent years, the market growth of isoxazolone has benefited from the listing of Corvus. Corvus applied glyphosate to maize before sprouting. In 2013, the balance GT soybean jointly developed by Bayer and MS technologies in the United States was registered in the United States, which endows the soybean with tolerance to isoxazolone and glyphosate. Similarly, the product has been registered in countries such as Canada and Brazil, and has obtained import licenses from the European Union, Australia and New Zealand. In July 2018, Bayer and MS technologies launched GM herbicide tolerant soybeans libertylink gt27 (fg72 × ll55) in the United States. This soybean has tolerance to glyphosate, glyphosate and isoxazolone. Bayer said the soybean had obtained all the necessary international import licenses before being commercialized in 2019. The development of this technology will open up a new field for HPPD inhibitor herbicides, and also enable isoxazolone to be used after soybean cultivation, thus greatly expanding the application market of this product. LibertyLink GT27 is widely licensed in North America. Bayer points out that more than 100 seed companies have signed agreements with them to apply the technology to their brand seeds in 2019. When Bayer acquired Monsanto, in order to meet the anti-monopoly requirements, it had signed an agreement to sell most of its libertylink business to BASF. In August 2018, BASF completed a € 7.6 billion acquisition of Bayer's divestiture business, including the libertylink herbicide resistant technology. In 2016, the global sales volume of isoxazolone was US $220 million; the compound annual growth rate from 2011 to 2016 was 5.9%. Its market growth benefited from the control of resistant weeds and the launch of new products. Isoxazolone is mainly used in corn. In 2016, the sales volume of isoxazolone in corn was US $141 million, accounting for 64.0% of the global market; the sales volume of isoxazolone in sugarcane was US $41 million, accounting for 18.6% of the global market; other fruits and vegetables (US $8.23 million), cotton (US $2.98 million) and grains (US $400000) were also used in a small amount. Isoxazolone is mainly found in the United States (US $51 million; 23.2%), Brazil (US $51 million; 23.0%), Romania (US $23 million; 10.7%), France (US $16 million; 7.4%), Italy (US $14 million; 6.6%), Australia (US $11 million; 5.2%), Argentina, Czech Republic, Bulgaria, Hungary, Poland, Canada and Croatia , Serbia, Uruguay, South Africa, Spain, Mexico, Russia, Bolivia, Chile, Slovakia, Turkey, Ukraine, Kenya, Austria, UK and other countries.
Registration status of isoxazolone
In May last year, the European Commission passed a review and approved the renewal of isoxazolone. The approval will take effect on August 1, 2019 and expire on July 31, 2034. After reexamination, the content of isoxazolone increased from 95% to 97.2%. The approved preparation product is 240 g / L isoxazolone suspension, registered for sweet corn only. During the re evaluation process, EU reminded Member States to pay special attention to: (1) the metabolites are related to the toxicity of groundwater, and attention should be paid to the protection of groundwater when using; (2) the long-term risks to mammals and the effects of processing on the properties of residues should be paid attention to during the preparation evaluation. At present, there are 12 effective registration of isoxazolone containing technical drugs / preparations in China: in terms of technical drugs, except Bayer, there are 3 registration of isoxazolone obtained in 2018; in terms of preparations, 7 Registration of suspension containing isoxazolone and 1 registration of water dispersible granule are only registered for corn fields. At present, a large number of pharmacodynamic tests have been carried out on isoxazolone in China, which provides a market-oriented basis for the promotion and application of this product in China.
BASF alite 27 (isoxazolone) has been approved by EPA for expansion registration
Recently, Agro pages world agrochemical network reported that BASF alite? 27 herbicide (active ingredient is isoxazolone) has been registered and approved by the U.S. Environmental Protection Agency and can be used in soybean fields in some counties of Indiana, Kansas, Kentucky, Missouri, Ohio, South Dakota and Tennessee. The registration is valid for 5 years until March 25, 2025. Alite? 27 is the first and only herbicide available for the libertylink gt27 soybean. "We have learned from farmers all over the country that there must be new ways to control economically damaging weeds," said the assistant director of EPA's office of chemical safety and pollution prevention According to the study of stratus AG, nearly 75% of the country's growers are facing the problem of glyphosate resistant weeds, of which 58% of the weeds in the fields of growers are resistant to other ways of action. With alite 27, growers will have a new way of acting and will be able to weed in soybean fields where libertylink gt27 is grown. As a part of libertylink gt27 soybean system, alite 27 herbicide will bring extraordinary advantages to growers compared with traditional pre seedling herbicide projects: - reactivation: alite 27 herbicide has excellent residual control over early season weeds and broad-leaved weeds, and can reactivate and remove weeds even when the hybrid plants are grown. -Reliable residual control: when mixed with other residual herbicides, alite 27 can provide more consistent, safe and broad-spectrum control for broad-leaved and gramineous weeds. -Drug resistance management: alite 27 herbicide has low usage and strong compatibility with pot mixing, and can be mixed with other pre seedling herbicide tanks to improve the herbicide resistance. "One of the biggest challenges for growers is resistance to weeds, and the soybean market needs a new active ingredient to deal with them," said Darren Holland, marketing manager, BASF agricultural solutions. The president of the American Soybean Association also said: "safe and effective weed management is a continuous challenge for farmers, and the expansion of isoxazolone registration will provide soybean growers with important new tools to fight destructive weeds and help better control emerging herbicide resistance problems." The American Soybean Association thanked the EPA for its efforts. In addition to controlling some of the most difficult weeds in soybean planting, isoxazolone can also effectively control the weeds that are already resistant to glyphosate. The United States is the second largest exporter of soybeans. In the United States, soybeans cover tens of millions of acres, with a total output value of billions of dollars. It is the main animal feed and one of the main sources of vegetable oil. "Soybean is a very important agricultural product for the United States and the world, and the use of isoxazolone component in transgenic soybean is expected to become an important measure of weed resistance management in the United States," said Shen Hua. This expansion will increase the demand of isoxazolone products in the United States, which is also worthy of continuous attention of soybean importing countries in the United States. "
Bayer launched "revolutionary" sugarcane herbicide Provence total in Brazil
At present, herbicide resistance has become an urgent problem to be solved in modern agricultural production in Brazil, and sugarcane industry is no exception. The longer the coexistence time of resistant weeds and crops, the greater the impact on sugarcane yield. 90 days before sugarcane growth cycle, weeds have an impact on sugarcane yield