1 Development of the Innovation System

1.1 Status of the Development of New Pesticide R&D Platforms in China

Over the past fifteen years, China has significantly increased its investment in the discovery and development of new pesticides and has established a number of national-level platforms for pesticide-related scientific and technological innovation. Supported by various national innovation systems, these platforms have begun to forge an R&D framework and innovative methodologies for the independent development of novel pesticides (see figure). 1) and, on this basis, developed a number of proprietary cultivars.

The following provides a brief overview of the key features of China’s new‑pesticide innovation system.

1.1.1 National-Level Platform for Pesticide Science and Technology Innovation

(1) National Southern Pesticide Innovation Center

The center was established in In 1995, and officially commissioned in January 2001 following acceptance by the Ministry of Science and Technology, the center comprises four research bases located in Zhejiang, Shanghai, Jiangsu, and Hunan. Its primary mission is to address the critical national need for green pesticides by tackling two key scientific challenges—identifying novel lead structures and elucidating molecular targets—and thereby establishing an innovative research framework for pesticide discovery that integrates biological knowledge, computational methods, and state-of-the-art chemical synthesis techniques. Building on this foundation, the center conducts the discovery and development of new low‑dose, ultra‑high‑efficacy, environmentally friendly pesticides, providing both theoretical and technical guidance to overcome bottlenecks in China’s independent innovation in pesticide R&D, and laying a solid theoretical and technological groundwork for green pesticides to support sustainable environmental, ecological, and agro‑industrial development in China.

(2) National Engineering Research Center for Pesticides

The center was approved by the State Planning Commission and established at Nankai University in… Construction began in 1996, with the Nankai University Institute of Element‑Organic Chemistry serving as the project developer. In 2001, the National Development and Reform Commission approved the establishment of the Shenyang Center. The primary mission and objectives of the National Engineering Research Center for Pesticides are to pioneer the discovery of novel pesticides, conduct research on their development, carry out engineering‑scale studies, and facilitate the translation of scientific findings into productive applications.

(3) State Key Laboratory of New Pesticide Creation and Development

The State Key Laboratory for the Creation and Development of New Pesticides, based at the Shenyang Research Institute of Chemical Industry, is committed to ensuring that China’s pesticide research—beginning at the molecular design stage—rigorously incorporates environmentally friendly criteria. From start to finish, it integrates safety and environmental assessments of novel chemical structures, promotes the development of ultra‑high‑efficacy pesticides, and seeks to significantly mitigate environmental impacts. The laboratory also pursues new active ingredients with innovative functions and mechanisms of action, addressing existing limitations and enhancing compatibility with the environment. In parallel, it places particular emphasis on the study of plant‑regulating substances, exploring ways to control the growth, development, and reproduction of harmful organisms while improving bioselectivity. By making technological innovation a central pillar, the laboratory keeps abreast of cutting‑edge international developments, striving to position China as a nation capable of inventing new pesticides with independent intellectual property rights.

(4) National Engineering Research Center for Pesticide Innovation

The National Engineering Research Center for Pesticide Innovation is In December 2005, with approval from the Ministry of Science and Technology, a national-level engineering technology research center was established, based on the Hunan Institute of Chemical Research. The center primarily conducts research and development, as well as technical services, in such fields as novel pesticide discovery, scale-up production of active ingredients and intermediates, pesticide product chemistry, pesticide residue analysis, ecotoxicology, environmental behavior, pesticide biology, chemical analysis and testing, and metrological verification of instruments and equipment.

(5) National Engineering Research Center for Biological Pesticides

The center is affiliated with the Hubei Academy of Agricultural Sciences and was established in… On January 7, 2011, this biopesticide engineering technology research institution was approved by the Ministry of Science and Technology. The laboratory primarily conducts research on critical and common technologies for biopesticides and, based on the integration of relevant technological achievements, undertakes engineering and industrialization development studies. Ultimately, it aims to establish a technical platform for the research, production, and application of biopesticides—both in China and internationally—and to serve as a training base for related R&D talent, thereby providing crucial technical support for the sustainable development of China’s biopesticide industry.

(6) National Key Laboratory Cultivation Base for Green Pesticides and Agricultural Bioengineering

This breeding base is supported by the Center for Research and Development of Fine Chemicals at Guizhou University. Its laboratories focus on addressing critical challenges that constrain China’s food security, the control of agricultural pests and diseases, and the quality and safety of agricultural products. Guided by the region’s biological resources, the center conducts research in green pesticide discovery and molecular target identification, sustainable pest‑management technologies, pesticide analysis and environmental impacts, and green synthesis methodologies.

1.1.2 Provincial and Ministerial-Level Pesticide Science and Technology Innovation Platform

In addition to the aforementioned national-level platforms for the development of new agrochemicals, China has also established a number of provincial- and ministerial-level laboratories dedicated to the creation of novel pesticides, which primarily include:

① The Key Open Laboratory of Pesticide Chemistry and Applied Technology of the Ministry of Agriculture, jointly established by the Institute of Plant Protection of the Chinese Academy of Agricultural Sciences and the College of Science of China Agricultural University;

② Relying on the Key Laboratory of Natural Pesticides and Chemical Biology of the Ministry of Education at South China Agricultural University, the institute primarily conducts research in areas including botanical pesticides, plant protection agents, pesticide residues and environmental toxicology, resistance mechanisms and management in harmful organisms, formulation development and application of pesticides, pesticide biotechnology, as well as the design and synthesis of new pesticides.

③ The Key Laboratory of Green Pesticides and Agricultural Bioengineering, established under the auspices of the Center for Research and Development of Fine Chemicals at Guizhou University, primarily conducts research in areas including green pesticide design and synthesis, target identification and mechanism of action, process route development for green pesticides and functional molecules, pesticide analysis and environmental impacts, and the sustainable management of major crop diseases and pests.

④ Relying on the Key Laboratory of Pesticide and Chemical Biology of the Ministry of Education at Central China Normal University, the research primarily focuses on molecular design and synthesis of green pesticides, organic process route engineering in the development of novel pesticides, pesticide residue analysis and environmental chemistry, as well as molecular biology related to pesticide pharmacology.

⑤ Relying on the Ministry of Education Engineering Research Center for Plant Growth Regulators at China Agricultural University, this center was established by integrating internal and external resources on the basis of the university’s Crop Chemical Control Research Center. It is currently the only ministry-level engineering research center in the field of plant growth substances.

⑥ The Strategic Alliance for Technological Innovation in the Pesticide Industry, established in April 2010, aims to advance technological progress in the pesticide sector. It is a voluntary association of enterprises and institutions engaged in the research, development, production, manufacturing, and services related to active ingredients, intermediates, formulations, adjuvants, and other associated products.

1.2 Development of China’s New Pesticide Innovation System

From Since the Seventh Five-Year Plan period (1985–1989), China has possessed domestically developed agrochemicals. However, the country’s efforts to create new pesticides truly took off during the Ninth Five-Year Plan period, when the establishment of two pesticide‑innovation centers—one in the north and one in the south—marked the formal launch of research on pesticide discovery and development. During the Tenth Five-Year Plan period, the focus shifted to conducting research on the creation of novel pesticides and developing key technologies for their industrialization. The Eleventh Five-Year Plan centered on a “Pesticide Innovation Project.” Building on this earlier work, the Twelfth Five-Year Plan saw the implementation of the National Science and Technology Support Program and the “Research, Development, and Industrialization of Green and Ecological Pesticides” project, which primarily aimed at advancing the industrial-scale development of previously identified candidate compounds.

In addition, the National Natural Science Foundation of China Projects such as the National Natural Science Foundation of China (NSFC), the 973 Program, and the 863 Program have also provided substantial financial support for the development of new pesticides in China. With this funding, China has made initial progress in fundamental theoretical research on new pesticides and in the study of innovative methods for their discovery, thereby establishing a nascent theoretical framework and methodological foundation for scientific and technological innovation in this field.

1.3 Major Institutions in China Engaged in the Development of New Pesticides

At present, the main entities engaged in the development of new agrochemicals in China include universities and certain research institutes, while a small number of enterprises have also begun to undertake such efforts.

1.3.1 Higher Education Institutions

At present, the major Chinese universities engaged in the development of new agrochemicals include Guizhou University, Nankai University, Central China Normal University, East China University of Science and Technology, China Agricultural University, Northwest A&F University, Shanghai Jiao Tong University, Zhejiang University of Technology, Nanjing Agricultural University, and others; all of these institutions have achieved some degree of commercialization of their products. In addition, other institutions, such as Shanghai Normal University, have also undertaken active research efforts in the discovery and development of novel agrochemicals.

1.3.2 Research Institutes and Institutions

In China, numerous research institutes are also engaged in the development of new agrochemicals, and many have been restructured into enterprises. The key companies involved in the creation of novel pesticides include: Jiangsu Institute of Agrochemicals, Hunan Chemical Research Institute, Shanghai Institute of Agrochemicals, Dalian Institute of Chemical Physics of the Chinese Academy of Sciences, Shenyang Chemical Research Institute, Sichuan Chemical Research Institute, Zhejiang Chemical Research Institute, Institute of Process Engineering of the Chinese Academy of Sciences, and Shanghai Institute of Organic Chemistry of the Chinese Academy of Sciences, among others.

1.3.3 Enterprises

(1) Major Enterprises Involved in the Development of New Pesticides At present, very few enterprises in China are engaged in the development of new pesticides. Aside from a number of research institutes that have transitioned into corporate entities, only a handful of companies—such as Zhejiang Longwan, Dalian Ruizé, Jiangsu Yangnong, and Shandong Zhongnong United—are conducting independent research and development of novel pesticides.

(2) The Role of China’s Pesticide Companies in the Development of New Pesticides Due to the high capital requirements and significant risks associated with new‑pesticide development, most Chinese pesticide firms are reluctant to invest in such research, preferring instead to vie for patents that are about to expire. This inevitably places domestic pesticide companies at a competitive disadvantage. Nevertheless, a small number of Chinese enterprises have already undertaken R&D on novel pesticide compounds; although their structures may not be particularly innovative, these companies have recognized the drawbacks of operating without patent protection. Prior to the transformation of research institutes, only a handful of firms were engaged in pesticide innovation. However, as some research institutions undergo restructuring, enterprises are poised to become the main driving force behind new‑pesticide development in China. For instance, institutions such as the Shenyang Research Institute of Chemical Industry and the Hunan Research Institute of Chemical Industry have seen a marked increase in the number of newly registered pesticides in recent years, emerging as key players in China’s new‑pesticide R&D landscape.

2 Innovative Technology Development

For a long time, Chinese scholars have lagged behind in research on theoretical models for the discovery of new agrochemicals, lacking sufficient influence and seeing their work rarely recognized by the international academic community as mainstream frameworks. In recent years, however, Chinese researchers have achieved notable progress in areas such as the identification of novel targets and lead compounds for antifungal and antiviral agents, as well as in the development of related theories and methodologies. They have proposed several original models and approaches, thereby exerting a significant impact on the global scientific community.

2.1 Intermediate Derivatization Method

Professor Liu Changling of the Shenyang Research Institute of Chemical Industry has innovatively proposed a unique… “The Intermediate Derivatization Approach,” for which the author was invited to contribute an article titled “Application of the Intermediate Derivatization Approach in Agrochemical Discovery” to the internationally renowned journal Chemical Reviews, provides a detailed exposition of the essence and applications of this novel pesticide‑innovation methodology. The paper presents numerous examples demonstrating how this approach has been used to develop new agrochemical candidates. By optimizing key metrics such as development time, investment, and efficiency, it has significantly increased the success rate of new‑pesticide discovery, offering a fresh methodological framework and innovative perspective that enhances both the quality of drug‑discovery efforts and awareness of intellectual‑property protection, while improving the hit rate of candidate compounds. With its substantial potential, the IDMs (Intermediate Derivatization Method) has garnered widespread attention from the international scientific community in both pharmaceutical and agrochemical R&D.

The intermediate derivatization method, from a chemical perspective, simplifies complex problems and delivers excellent results. It comprises three key components (as shown in the figure). As shown in Figure 2, the approaches are as follows: ① Employing intermediates in chemical reactions to design and synthesize novel compounds, followed by screening to identify lead compounds, which are then optimized to yield new agrochemicals; ② Starting from simple starting materials, synthesizing new intermediates via chemical reactions, and using these intermediates to replace specific structural fragments in known agrochemical or pharmaceutical molecules, thereby generating new compounds that, upon further investigation, evolve into new agrochemical products; ③ Utilizing known bioactive compounds or established agrochemicals as intermediates, conducting chemical transformations to design and synthesize new compounds, and ultimately identifying new agrochemicals through screening and optimization studies. This strategy has successfully led to the development of fungicides such as azoxystrobin, cyprodinil, and pyraclostrobin, delivering significant economic and social benefits. Notably, azoxystrobin was awarded the Excellent Prize of the China Invention Patent Award and the First Prize of the 2014 Technology Invention Award from the China Petroleum and Chemical Industry Federation. Meanwhile, the acaricide pyrimidifen and the fungicide bixafen are currently undergoing registration procedures, while insecticidal compounds SYP‑3409 and 4380, the fungicide 9069, the insecticidal–acaricidal compound 2260, the acaricide 4523, and the herbicide 2194 are also under active research and development.

2.2 A Novel Approach to Lead Discovery Based on Molecular Three-Dimensional Shape and Pharmacophore Features

East China University of Science and Technology has proposed a method for identifying novel bioactive scaffolds through scaffold hopping, based on similarity comparisons of molecular three-dimensional shapes and pharmacophore features. This approach comprehensively accounts for the advantages and limitations of both feature-based and shape-based molecular superposition, which is of great significance for enhancing the hit rate in virtual screening and improving the efficiency of scaffold hopping. Using this method, East China University of Science and Technology has obtained nearly… Two hundred active scaffolds have laid a solid foundation for the discovery of new structures in subsequent research.

2.3 Drug Molecular Design Based on Bioactive Fragments

Zhao Weiguang and colleagues at Nankai University have proposed a method for discovering new agrochemicals by leveraging the structures of known active fragments and integrating computer-aided drug design approaches to carry out rational molecular design. They have put forward a novel… “Drug molecule design based on pharmacophores” (Figure 4) eliminates reliance on the three-dimensional structure of proteins. By extracting pharmacophoric motifs from the structures of existing cellulose synthase inhibitors and incorporating a di‑alkoxyphenyl moiety into valine amide–based compounds, they identified highly active candidates. Further enhancing the conformational flexibility of these compounds led to the discovery of several analogs with activity surpassing that of enilconazole.

To be continued~