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chirality： Chirality，The word comes from cheir, Greek ，An object cannot coincide with its mirror image。 Chirality is the basic property of three-dimensional objects. If an object cannot coincide with its mirror image, it is called a chiral object. It is a common three-dimensional geometric relationship, which is ubiquitous in nature, ranging from galaxies to molecules. It can be said that chirality is the basic attribute of nature. There are a wide range of chiral relationships in life. Chirality is of far-reaching significance in the field of medicine. Among the new chemical entities (NCE) approved every year, the proportion of chiral drugs is increasing year by year.
手性药物： The human body environment is chiral, and different chiral compounds may play different roles in human body. The U.S. Food and Drug Administration (FDA) stipulates that the stereoisomers of chiral drugs should be obtained respectively when conducting pharmacological and toxicological studies on chiral drugs, and necessary comparative studies should be carried out to determine the drugs to be further developed. At the same time, it is pointed out that the other enantiomers are impurities. Therefore, the development of chiral drug preparation technology becomes the key.
Asymmetric hydrogenation technology： Asymmetric hydrogenation technology emerged in the 1970s, and now it has developed to the fourth generation. It has the characteristics of green, environmental protection and energy saving, and can efficiently prepare chiral drugs. After more than 30 years of development, it has gradually changed from scientific exploration of laboratory to industrial application. A new high-tech industry is emerging. At the same time, people also increasingly realize the importance of chiral technology for human health and ecological environment. In 2001, Nobel Prize in chemistry awarded three scientists who are engaged in asymmetric catalytic synthesis, noels, yeeliaki and sharp rice, to reward their outstanding contributions in the basic and applied research of asymmetric catalytic hydrogenation and oxidation. However, because of its high technology content and high barriers, it has not been widely used in commercialization until nearly 20 years, and it reflects its great advantages in environmental protection, safety, cost and other aspects, as well as economic, environmental protection and social value. At present, more than 75% of the small molecule drugs in the world are chiral drugs, and 60% of them can be obtained by asymmetric hydrogenation technology. Chiral catalyst is the core problem of efficient green synthesis of drugs. Therefore, asymmetric hydrogenation technology plays an important role in the synthesis of pharmaceutical raw materials and intermediates, and its wide application will have an important impact on the pharmaceutical industry, It is bound to affect the future pattern of the industry.
Development of asymmetric hydrogenation technology
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