On the "previous life and life" of oxazolin

"Power" and "Ai Xiu" are not strangers to the country. This is the two wheat herbicides that Syngenta currently pushes in China. With the increase of resistance to grassy weeds in the wheat field in recent years, the control of weeds in wheat fields has become more and more serious. The two products “Daeng” and “Ai Xiu” are currently selling very hot in China, mainly because they have excellent control effects on grass and weeds in wheat and wheat fields. Here, I will lead you through the "previous life and life" of the main active ingredient of these two products - oxazolin.

Pinoxaden is a new phenylpyrazoline herbicide developed by Syngenta. It is also an acetyl-CoA carboxylase (ACC) inhibitor herbicide. Oxaloxacin is mainly used to control annual grass weeds in wheat and wheat fields, and grass weeds such as wild oats, ryegrass, foxtail, hard grass, valerian, maiden, japan, and genus It has good control effect, especially for some malignant grass weeds such as wild oats, ryegrass, hard grass and valerian, which are close to 100%. In addition, it has high safety to wheat and barley, and it has a wide application period (can be applied from the 2nd leaf stage to the booting stage of wheat seedlings). These characteristics make the oxazolin ester very fast since its launch. development of.

In 2005, oxazolin was registered and marketed under the trade name Axial in the United States and the United Kingdom, which is the first appearance of oxazolin on a global scale. Subsequently, oxazolin was successively registered in countries such as India, Germany, Italy and Canada. In 2009, oxazolin was temporarily registered in China and officially registered at the end of 2010 for winter wheat and spring wheat and wheat fields to control grass weeds. Since its launch, the product has developed extremely rapidly, and it can be said that market development has been quite successful. In 2007, the third year after the listing of oxazolin, its global sales easily broke through the $100 million mark and successfully entered the multi-billion dollar club. In 2008, oxazolin was one of the two most important products in Syngenta's new products. In 2014, the global sales of oxazolin was US$425 million, which became one of the top 10 products of Syngenta sales in the year, and it is one of Syngenta's five herbicides (others have mesotrione and glyphosate). , paraquat and metolachlor). Zodialin is currently the most important member of the Syngenta Cereal Herbicide product line, and Syngenta will spare no effort in the in-depth development of this product (probably mainly with multiple products), the future The development space is still very large.

For the time being, oxazolin is used in two main areas worldwide, in the cereal sector (mainly wheat and barley) and in non-crop areas. Cereals are the main application crop for oxazolin. In 2014, sales of oxazolin on cereals reached $250 million, accounting for 60% of the total sales of oxazolin. Non-crops (turf and horticulture, etc.) are another major area of ​​use of oxazolin, especially in Europe and North America. In 2014, oxazolin was sold in the field of US$170 million, accounting for 40%. However, Syngenta does not currently release oxazolin in this field in China, which is a future growth point for oxazolin.

Since its first registration in the United States in 2005, the registration footprint of oxazolin has spread to more than 50 countries in Europe, South America, North America, Asia Pacific and South Africa. As far as the market for oxazolin is concerned, it is distributed in the major cereal growing countries in the world, but the two most important markets are North America and Europe. Zoolarin is currently the most important cereal herbicide variety in Europe and North America, with annual sales in both regions above $100 million. In the Asia-Pacific region, oxazolin is mainly distributed in cereal crops in China and Australia, especially in the Chinese market. Syngenta's promotion of this product is currently hot. In addition, although the sales of oxazolin are not high in Latin America, the development in recent years is obvious. At present, oxazolin has become a cereal crop in Argentina and other countries except glyphosate and 2,4-D. The largest herbicide variety.

In most markets around the world, Syngenta is the only registered holder of the original oxazolinic acid and is the majority of the registration holders (in some countries, such as the United Kingdom, Syngenta grants the original drug to local companies for development). preparation). In terms of registered products, Syngenta has registered a large number of single-agent and compound products worldwide (see Table 1 for details). The oxazolin ester is mainly compounded with a safener or a herbicide such as oxalate, diflufenacil, flufenoxyacetic acid or clodinafop, and the common dosage form is emulsifiable concentrate. In China, Syngenta is still the holder of the original drug and preparation of the oxazolin, registered 95% of the original drug, and 5% oxazolinol emulsifiable concentrate (Ai Xiu) and 2.5% oxazolin + 2.5% Acetyl oxalate emulsifiable concentrate (power). But at this stage, many companies in China have started field trials of oxazolin. According to official information from ICAMA, there are currently 15 domestic companies that have applied for 16 field trials. The applied preparations are mainly 5% oxazolinol emulsifiable concentrate (8) and 2.5% oxazolinol + 2.5% acetylene oxalate. Dairy oil (3), and Anhui Jiuyi Agriculture and other three companies also applied for a new dosage form of dispersible oil suspension agent of oxazolin, as shown in Table 2.

Zyloxacillin is still in the patent protection period and belongs to Syngenta's patented product. Its patent numbers in Europe and the United States are EP1062217 and US6410480, both of which will expire on March 11, 2019. The SPC protection in Europe mainly protects the compound products of oxazolin and other active ingredients (2020) period). The patent number ZZ99803747.8 (3-hydroxy-4-aryl-5-oxopyrazoline derivative with herbicidal activity) of oxazolin in China will also expire on March 11, 2019. At the time when the patent is about to expire, several companies in China have begun to develop this product. As far as the future trend of the product is concerned, according to the consistent style of the multinational company, the product after the patent expires will be compounded with its patented product to extend the exclusive life of the product. If domestic companies want to take a slice from Syngenta, they can develop a compound preparation of oxazolin and other safeners or herbicidal active ingredients, or develop new dosage forms to replace existing emulsifiable formulations, or find new markets. Breakthrough points, such as focusing on non-crop areas.

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