The National Science and Technology Awards Conference was solemnly held in Beijing on the morning of Jan 10th, 2020. The project "Discovery of Highly Efficient Chiral Spiro Catalysts" (mainly completed by: Zhou Qilin, Xie Jianhua, Zhu Shoufei, Wang Lixin) led by Zhou Qilin, an academician of the Chinese Academy of Sciences and a professor of College of Chemistry, Nankai University, won the first prize of the National Natural Science Award. This is also the only project that won the first prize of the National Natural Science Award this year. At the Conference, President Xi Jinping presented the award to Zhou Qilin.

"Mirrored but not superimposable", this is a phenomenon that is ubiquitous in nature, ranging in size from cosmic nebulae to molecular structures. Molecules of different chirality have similar structures but different properties. Among the drugs used for treatment, many are chiral molecules, and the different enantiomers of chiral drugs usually show different effects in physiological processes. However, in general chemical synthesis, these two enantiomers of the chiral molecules appear in equal proportions, so for every kilogram of drug produced, the pharmaceutical company has to struggle to separate the half one. It is the dream and pursuit of chemists to create chiral molecules as accurately and efficiently as what enzymes do. Asymmetric catalysis was thus born and has become the most effective method to create chiral molecules. And that’s what the Prof. Zhou and his teammates have been working for.

After 20 years of continuous efforts, Prof. Zhou Qilin, with his research group, has developed a new kind of chiral spiral ligands with spirobiindane skeleton. Based on the skeleton, a series of chiral spiral catalysts have been designed and synthesized, which showed high catalytic activity and excellent enantioselectivity in many asymmetric reactions, and still keep records as catalysts with the highest catalytic activity and enantioselectivity in many reactions. In particular, the urnover number of the ultra-efficient chiral spiral-iridium catalyst has reached 4.5 million in the asymmetric catalytic reaction of ketones, making it the most efficient chiral molecular catalyst to date.

In the process of developing chiral spiral catalysts, Prof. Zhou and his team systematically developed the design method of chiral catalysts, and proposed the idea of improving the chiral induction ability and stability of catalysts with rigid framework. Recently, Zhou’s group also developed the asymmetric insertion of metal carabines to heteroatomic-hydrogen bonds in high regioselectivity and high yields (using a Pybox-copper and Pybox-iron as catalysts), which was widely thought as low-reactive reactions.

Thanks to Prof. Zhou and his team’s work, chiral spiro ligands have been commercialized and widely used in the syntheses of chiral compounds and the productions of chiral drugs, and have significantly promoted the development of synthetic chemistry.