Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy , Ocean University of China , Qingdao 266003 , China.
Laboratory for Marine Drugs and Bioproducts of Qingdao National Laboratory for Marine Science and Technology , Qingdao 266003 , China.
Org Lett. 2018 Nov 2;20(21):6682-6686. doi: 10.1021/acs.orglett.8b02731. Epub 2018 Oct 24.
Following the reactivity inversion strategy, two different two-step sequences were designed and successfully applied to the asymmetric synthesis of spiro-bridged and spiro-fused heterocyclic compounds, which combined chromane, indole, and oxindole, three potential pharmacophores, in one molecule. The power of these two organocatalytic pathways is underscored by mild reaction conditions and high efficiency in the production of synthetically challenging, but biologically important heterocyclic products, which could be transformed into more biologically interesting heterocyclic structures.
采用反应反转策略，设计并成功应用了两种不同的两步序列，实现了将色满、吲哚和氧吲哚三个潜在药效团结合在一个分子中的螺桥和螺稠合杂环化合物的不对称合成。这两种有机催化途径的优势在于反应条件温和，高效合成具有挑战性但具有生物重要性的杂环产物，这些产物可以进一步转化为更具有生物意义的杂环结构。
