作者
Tie–Gen Chen, Lisa M Barton, Yutong Lin, Jet Tsien, David Kossler, Iñaki Bastida, Shota Asai, Cheng Bi, Jason S Chen, Mingde Shan, Hui Fang, Francis G Fang, Hyeong-wook Choi, Lynn Hawkins, Tian Qin, Phil S Baran
发表日期
2018/8/16
期刊
Nature
卷号
560
期号
7718
页码范围
350-354
出版商
Nature Publishing Group UK
简介
Prized for their ability to rapidly generate chemical complexity by building new ring systems and stereocentres, cycloaddition reactions have featured in numerous total syntheses and are a key component in the education of chemistry students. Similarly, carbon–carbon (C–C) cross-coupling methods are integral to synthesis because of their programmability, modularity and reliability. Within the area of drug discovery, an overreliance on cross-coupling has led to a disproportionate representation of flat architectures that are rich in carbon atoms with orbitals hybridized in an sp2 manner. Despite the ability of cycloadditions to introduce multiple carbon sp3 centres in a single step, they are less used. This is probably because of their lack of modularity, stemming from the idiosyncratic steric and electronic rules for each specific type of cycloaddition. Here we demonstrate a strategy for combining the optimal features of …
引用总数
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