China has been a great agricultural country since ancient times, and the prosperity and development of agriculture is the material foundation of Chinese civilization. Since the founding of the People's Republic of China, China's population has been increasing and its cultivated land area has fluctuated. In the past ten years, it has remained at about 2 billion Mu, while China's Food self-sufficiency ratio has been decreasing year by year (already below 90% of the world's safety standards) , large quantities of food are imported from abroad every year. How to increase grain output has become the most important problem in China's agricultural development. Increasing the area of cultivated land is very difficult, so increasing the yield and quality of grain per unit area has become a crucial solution. Although there are many measures to improve the yield per unit area, the application of pesticide is a measure with a high input-output ratio (up to 1:20) , which can not only effectively control the diseases, pests and weeds, but also increase the yield per unit area, it improves the quality. According to the statistics of the Food and Agriculture Organization of the United Nations, about one third of the world's grain production is lost every year due to diseases, pests and weeds. Without control measures, the loss rate of agricultural production is over 40% , or even no harvest. And every year through plant protection measures such as prevention and control of diseases, pests and weeds, the losses recovered can reach about 200 billion catties, accounting for more than 15% of the total output. Therefore, modern agriculture can not do without pesticides.
Although China is one of the earliest countries to use pesticide, the research and application of modern pesticide innovation were introduced from the West, which started later than European and American countries. Since founding ceremony of the People's Republic of China, the level of pesticide production in China has been continuously raised, and so far, the production capacity has reached the world's leading level. Although the production capacity is very strong, but the ability of innovation is still relatively weak, mainly because new pesticides are difficult to create, and new varieties must meet the "efficient, safe, economic" requirements. The difficulty of pesticide creation can be seen in the fact that, according to Phillips McDougall, 12 years of work is required to screen an average of 160,000 compounds for the successful launch of a new pesticide. New Pesticides need more and more compounds to be screened, more and more expensive, and more and more time to develop. New Varieties not only require better results, but also are safer than existing products and have more significant cost-effective advantages, many of the candidate compounds pass muster as active, but fall at the feet of safety or cost-effective. And there is also the problem of resistance, due to the strong reproductive capacity of agricultural pests (such as the Cotton Aphid can reproduce 7 to 10 generations a year, the MITE can reproduce 30 to 40 generations) , grass damage is also mostly annual weeds, if the use of inappropriate methods or inappropriate application of time, this leads to resistance to pests and weeds; for example, new acaricides often have a lifespan of only five years due to the emergence of resistant Mites. In addition, with the increasing public demand for safety risk assessment and the improvement of pesticide registration standards, it is becoming more and more difficult to create and develop new pesticides. Because of this, up to now, there are only about 50 kinds of pesticide in China, and there are only about 10 kinds of pesticide in large area. Nevertheless, compared with more than 600 varieties which are widely used in more than 2000 kinds of pesticide invented in foreign countries, they are basically the same.
There are six levels of innovation in the creation of new pesticides: The first is the study of known compounds and the discovery of their uses or new uses, or the use of known intermediates as active ingredients; the second is the selective invention of compounds within the scope of patents, develop "me too" or "me better" new drugs; the third layer develops "me too" new drugs for compounds outside the scope of the patent; the fourth layer develops "me better" new drugs for compounds outside the scope of the patent; The fifth layer is for self-discovery of new structure and development of "me first" or "first in class" new drug; the sixth layer is for self-discovery of new structure and New Action Mechanism and development of "first in class" new drug. In general, the new pesticide varieties created in China have limited cost-effectiveness and are mostly "me too" . Although they can be patented, their patent rights are not stable and they are not competitive with those of large foreign companies. However, the European, American and Japanese pesticide giants are strong in new drug innovation and have a high level of technology. In the past 40 years, most of them have studied compounds of the 4th to 6th level. As a result, the compounds they invented have a new structure, a good effect and a significant cost-performance advantage, has a monopoly on the market.
Although there are many ways and methods to create new pesticides, we should keep pace with the times and innovate constantly. If the new pesticides in China want to be innovative in original structure or different in action mechanism from the existing ones, they can not be replaced by imitations of foreign ones or simple organisms, and they must have new innovative strategies, it is important to ensure that innovative products have stable intellectual property rights and to consider cost-effectiveness, as the registration fees alone will run into hundreds of millions of yuan (about 20 million yuan in China) and take five to eight years. In order to solve these problems, the author's team has established "intermediate derivatization method" after more than 20 years' exploration, practice and research, which can be used not only to study "me better" , but also to study new structural compounds, and the success rate of new pesticide innovation was greatly increased. This innovative approach differs from existing approaches in that development is considered at the same time as the design of pesticide molecules. Using cheap, safe and environmental-friendly raw materials (intermediates) to design new pesticide molecules beyond the scope of existing patent protection, after many rounds of "design-synthesis-test-analysis" research, the new pesticide candidates with good activity, high safety and good performance-price ratio were screened out. After years of practice and application by the team, more than 10 candidate new pesticide varieties have been selected from 30,000 compounds, of which 3 have been commercialized and many are under registration or development, for example, herbicides 1604 and fungicides 1602 have the potential to become hundreds of millions of dollars in sales "Blockbuster" ; Other companies, such as Qingdao Qingyuan Chemical Co. , Ltd. and Shandong United Pesticide Industry Co. , Ltd. , have also used this method to successfully create several new pesticide varieties, such as cyhalofluoxetone and fluoetheramide, it shows that the intermediate derivative method is universal and can greatly improve the success rate of new pesticide creation, shorten the development cycle and reduce the cost of research and development.
Current situation of pesticide in China
English
