Progress has been made in the study of γ-δ-endamide in the synth asymmetric synthesis of two-handed sex centers

Hand endamide is an important skeleton structure of bioactive compounds such as drugs and natural alkaloids.
At present, hand endamide is mainly synthesized by the chemical methods of Michael reaction based on C-C bond and catalytic asymmetric hydrogenation reaction of precious metals, which have more reaction steps, higher synthesis cost and difficult to popularize on a large scale.
The method of producing γ-or δ-endamide using an asymmetric amine-transaminase catalytic ketone ester is also used in a small number of applications, but this method can only form a hand center, how to accurately construct an efficient high-stereoscopic selective multi-hand center by enzymatic method, to obtain a single configuration of γ-or δ-endamide is still a difficult problem.
Zhu Dunming, a researcher at the Tianjin Institute of Industrial Biotechnology of the Chinese Academy of Sciences, and Wu Qiqing led a team of bio-catalytic and green chemicals who obtained high stereo-selective omega-transaminase through screening of laboratory enzyme banks, which not only catalyzed the formation of asymmetric C-N bonds, but also identified the hand of a-C, using omega-transaminase The stereo-recognition of ketone-based α-C, through spontaneous in-place cyclic reaction, realizes the precise construction of the two-handed center γ-or δ-endamide, the yield is 46-68%, the ee value is greater than 99%, and the proportion of non-reflective isomers is 99:1.
the study provided a new chemical-enzyme catalytic "one pot" strategy for asymmetrical synthesis of γ-or δ-endamides in two-hand centers.
research has been supported by the National Natural Science Foundation of China and the Tianjin Science and Technology Commission.
study was published in ChemCatChem.
Wenxuan, an assistant researcher at Tianjin Institute of Technology, is the first author of the thesis and Zhu Dunming is the author of the paper newsletter.
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