N-苄基马来酰亚胺与烯烃的[2+2]光环加成反应：一种合成功能性3-氮杂双环[3.2.0]庚烷的方法
[2+2]-Photocycloaddition of N-Benzylmaleimide to Alkenes As an Approach to Functional 3-Azabicyclo[3.2.0]heptanes.
作者信息
Skalenko Yevhen A, Druzhenko Tetiana V, Denisenko Aleksandr V, Samoilenko Maryna V, Dacenko Oleksandr P, Trofymchuk Serhii A, Grygorenko Oleksandr O, Tolmachev Andrey A, Mykhailiuk Pavel K
机构信息
Enamine Ltd. , Chervonotkatska 78 , Kyiv 02094 , Ukraine (www.enamine.net, www.mykhailiukchem.org).
Institute of High Technologies , Academician Glushkov av. 4G , Kyiv 03022 , Ukraine.
出版信息
J Org Chem. 2018 Jun 15;83(12):6275-6289. doi: 10.1021/acs.joc.8b00077. Epub 2018 Mar 12.
A one-step synthesis of functionalized 3-azabicyclo[3.2.0]heptanes by [2+2]-photochemical intermolecular cycloaddition of N-benzylmaleimide to alkenes was elaborated. The obtained compounds were easily transformed into the bi- and tricyclic analogues of piperidine, morpholine, piperazine, and GABA, which are advanced building blocks for drug discovery.
阐述了通过N-苄基马来酰亚胺与烯烃的[2+2]光化学分子间环加成一步合成功能化3-氮杂双环[3.2.0]庚烷的方法。所得到的化合物可轻松转化为哌啶、吗啉、哌嗪和GABA的双环和三环类似物，这些都是药物发现的先进构建模块。
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