The Xu Tao research group of Ocean University of China has made significant progress in the total synthesis of anti Alzheimer's drugs Galanthamine and Lycoramine.

Zhang Yuna: Recently, the Xu Tao research group of Ocean University of China has used the transition metal catalyzed inert bond activation strategy to complete the total synthesis of anti Alzheimer's drugs Galanthamine and Lycoramine The research results were published in organic letters (DOI: 10.1021 / ACS Orglett 9b04337) under the title of "total synthesis of galanthamine and lycoramine feeding an early stage C − C and a late stage dehydration via C-H activation" The work was selected as a cover article to push Galanthamine is an alkaloid isolated from lycoris, which has a significant reversible inhibitory effect on ache The hydrobromate of the compound was approved by the US FDA as the first choice drug for Alzheimer's disease in 2001 Because of its important physiological activity and challenging complex structure, many chemists at home and abroad are interested in its synthesis The total synthesis of galanthamine (source: Organic letters) from simple raw material 9, through the activation of RH catalyzed C-C bond, the author has successfully constructed four rings of ABCD in one step In particular, the reaction can achieve gram level preparation It is found that Beckmann rearrangement can be completed in the water phase In the later stage of the synthesis, the author activated C-H by one-step PD catalysis and introduced double bond regioselectively The synthesis of galanthamine was completed in 11 steps, and lycoramine was obtained from 15 ' The strategy of early C-C bond activation and late C-H bond functionalization has been demonstrated for the first time The first unit to complete this paper is the school of medicine, Ocean University of China Professor Xu Tao, the corresponding author, is the national "Qingqian", Haida "Zhufeng 3" Professor and Qingdao innovation leader The first author of this paper is Zhang Yuna, Ph.D student of Medical College, and Shen shuna, master's student, also participated in the work of this paper This work has been supported by NSFC general and major project subprojects, NSFC Shandong joint fund key projects and blue drug pool development plan project funds First author Zhang Yuna supplementary cover