通过 2-吡啶基乙酸酯与硝酮的去芳构化环加成反应，立体选择性和立体选择性合成功能化喹喔啉支架。
Diastereoselective and -Selective Synthesis of Functionalized Quinolizine Scaffolds via the Dearomative Annulation of 2-Pyridylacetates with Nitroenynes.
机构信息
Key Laboratory of Functionalized Molecular Solids, Ministry of Education, Anhui Key Laboratory of Molecule-Based Materials (State Key Laboratory Cultivation Base), College of Chemistry and Materials Science, Anhui Normal University, Wuhu, Anhui 241002, P. R. China.
出版信息
J Org Chem. 2022 Aug 5;87(15):9507-9517. doi: 10.1021/acs.joc.2c00448. Epub 2022 Jul 8.
An organocatalytic Michael/aza-Michael cascade reaction was developed to build the functionalized quinolizine scaffolds in 60-82% yields, excellent diastereoselectivities, and selectivities. This protocol involves the [3 + 3] annulations of 2-pyridylacetates with nitroenynes through the dearomative strategy in the presence of an organic base under mild conditions. The versatile late-stage derivatizations further demonstrated the synthetic utility of this methodology.
发展了一种有机催化的 Michael/aza-Michael 级联反应，以构建功能化的喹啉骨架，产率为 60-82%，具有优异的非对映选择性和选择性。该方案涉及在有机碱存在下，通过缺芳烃策略，在温和条件下，2-吡啶基乙酸盐与硝基烯炔进行[3+3]环加成反应。多样的后期衍生化进一步证明了该方法的合成实用性。
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