The "2021 International Summit Forum on Chemical Reaction and Pharmaceutical Technology", sponsored by the Organic Reaction and Process Branch Committee of the Chinese Chemical Society, was organized by Nankai University and Asymchem Pharmaceutical Group on September 17-18, 2021, bringing together more than 200 experts, scholars and researchers from domestic and foreign universities, research institutes and pharmaceutical enterprise. With the theme of "New Technologies, New Methods and Green Pharmaceutical Processes", it aims to promote academic exchanges and ideological collisions between academia and industry in the pharmaceutical industry to help accelerate the development of innovative drugs in China.
Academician Qilin Zhou, College of Chemistry of Nankai University and Dr. Yi Xiao, senior vice president of the Project Process Development Center of Asymchem Pharmaceutical Group, delivered opening remarks respectively. The meeting presented the latest scientific research achievements in different fields such as natural product synthesis, asymmetric synthesis, catalytic reaction, coupling reaction and technological innovation.
On the morning of September 17, Prof. Stephen Buchwald of MIT took the lead in sharing the course of developing CN coupling and the achievements of palladium catalytic reaction in new fields such as macromolecule and ADC coupling; Bin Zheng, director of Bristol Myers Squibb's Chemical Process Department, shared his work in pentavalent phosphorus chemistry, which made him win the 2021 Green Chemistry Presidential Award issued by the United States Environment Agency. Later, Prof. Zhen Yang of Peking University shared the story of developing chiral D-A reaction in natural product synthesis; researcher Qinghua Fan, Institute of Chemistry, Chinese Academy of Sciences, reported the achievement of chiral hydrogenation reduction of aromatic heterocycles, and skillfully used strong anion effect to synthesize many structural specific polycyclic chiral molecules; Prof. Wanbin Zhang of Shanghai Jiao Tong University, systematically introduced the angle regulation of catalysts in asymmetric synthesis, and the influence of weak interaction between catalysts and raw materials, as well as the application in the fields of chiral pentavalent phosphorus chemistry, the synthesis of drugs such as Redcevir artemisinin, and the catalysis of non precious heavy metals such as Co/Ni. Professor Aiwen Lei of Wuhan University shared the achievements in the field of optoelectronic coupling reaction. In pursuit of the spirit of perfect green reaction, he skillfully designed and replaced traditional organic oxidants with dots to achieve various C-X coupling reactions.
Dr. Xuecheng Jiao of Asymchem Biosynthesis Technology R&D introduced their achievements in biosynthesis technology and several application cases, which effectively improved the reaction efficiency by combining with continuous technology; Prof. Shoufei Zhu from the Nankai University shared the latest progress of chiral proton shuttles, with his unique achievements and insights on iron catalytic reaction it will inspire the further development of the application of iron catalysts; Prof. Li Deng of West Lake University introduced his experience in the design and development of weak bond catalysts; Ji Qi of Merck shared their technological strength of how to comprehensively analyze the reaction mechanism and pursue the optimal route design in the development of hepatitis C drugs; Yong Qin, professor of Sichuan University, shared three stories about the industrial full synthesis of complex natural drugs; Juntao Liu, director of process R&D of Baekje Shenzhou, introduced a R&D drugs process which had not yet been disclosed. The sharing and exchange of this front-end process is of significance for promoting the integration of production and research, and will also promote our respect for intellectual property rights.
In the international sharing on the second day, professor Jin Quan Yu of Scripps Research Institute shared the relevant topics of C-H activation such as stereoselectivity, positional selectivity and long-range projection control, showing unique achievements in ligand design and unlimited prospects for C-H activation; Bo Qu, senior chief scientist of Boehringer Ingerhan, introduced how to achieve efficient chiral hydrogenation of key aromatic heterocycles, which will continue to solve important problems in the field of catalysis in the future; Prof. Liuzhu Gong of the University of Science and Technology of China, shared the asymmetric allyl hydrocarbon functional groups; Prof. Wenjun Tang of Shanghai Institute of Organic Chemistry shared in detail the exploration results and application cases of the combination of square alkyl coupling; Prof. Gong Chen of Nankai University shared topics on cyclopeptide synthesis, chemical space exploration, and exploration and discovery of natural substrates.
Prof. Ning Jiao of Peking University shared and exchanged views on modification of active molecules and how to carry out innovative drugs around new targets, including discovery of new crown drugs; Fuhui Zhou of Hutchison Whampoa made a report with the research on the Suzuki reaction catalyzed by Na2PdCl4/DTBPPS in pure water; Prof. Hanfeng Ding of Zhejiang University discussed the research of natural products, the application of condition optimization electrochemistry in the [5+2] cyclization tandem reaction and the great prospect in the future; Prof. Wenjing Xiao of Central China Normal University shared the photo redox catalytic strategy in heterocycle synthesis and made exciting discussions and exchanges on the huge application prospects, especially in the context of carbon peaking and carbon neutralization; Yanfeng Zhang, chief scientific officer of Suzhou Jingyun, shared the crystal form screening and research strategies in the drug development process; Prof. Xinyuan Liu from Southern University of Science and Technology finally brought us the progress in the chiral anion copper catalyzed radical asymmetric cross coupling reaction.
How to apply new technologies and the latest academic achievements affects whether industry, universities and research can be truly integrated to a large extent. Academician Zhou Qilin mentioned that the forum will continue to provide a platform for exchanges between academia and industry in the future, hoping to accelerate the transformation of more recent research achievements through close exchanges.
