通过三组分串联反应合成1,4,5-三取代γ-内酰胺
Synthesis of 1,4,5 trisubstituted γ-lactams via a 3-component cascade reaction.
作者信息
Petersen Michael Åxman, Mortensen Michael A, Cohrt A Emil, Petersen Rico, Wu Peng, Fleury-Brégeot Nicolas, Morgentin Rémy, Lardy Claude, Nielsen Thomas E, Clausen Mads H
机构信息
Department of Chemistry, Technical University of Denmark, Kemitorvet 207, DK-2800 Kgs. Lyngby, Denmark.
EDELRIS, 115 Avenue Lacassagne, F-69003, France.
出版信息
Bioorg Med Chem. 2015 Jun 1;23(11):2695-8. doi: 10.1016/j.bmc.2015.01.041. Epub 2015 Jan 31.
A three component one-pot cascade reaction was developed for the synthesis of 1,4,5-trisubstituted γ-lactams. The resulting scaffold can be modified independently at three positions, two of which are conveniently accessed by changing the components of the one-pot reaction. The phases of building block generation, scaffold synthesis and subsequent appendage modification were adapted to library production, which resulted in a screening library of 500 compounds.
开发了一种三组分一锅法级联反应来合成1,4,5-三取代的γ-内酰胺。所得的支架可以在三个位置独立修饰，其中两个位置可通过改变一锅法反应的组分方便地实现。将构建块生成、支架合成及后续的附加修饰阶段应用于文库制备，得到了一个包含500种化合物的筛选文库。
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