State Key Laboratory of Natural Medicines (SKLNM) and Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University , Nanjing 210009, P. R. China.
Department of Organic Chemistry, China Pharmaceutical University , Nanjing 210009, P. R. China.
Org Lett. 2017 May 19;19(10):2596-2599. doi: 10.1021/acs.orglett.7b00914. Epub 2017 May 9.
A novel [3 + 3] cycloaddition between in situ formed azaoxyallyl cations and 2-alkenylindoles has been developed. This concise method allows the efficient construction of a series of tetrahydro-β-carbolinones in good yields under mild conditions. Gram-scale experiments and further derivatization of tetrahydro-β-carbolinones highlighted the potential utility of our method.
一种新型的[3 + 3]环加成反应,涉及原位生成的氮杂氧烯丙基阳离子与 2-烯基吲哚之间的反应,已经被开发出来。这种简洁的方法在温和条件下能够高效构建一系列四氢-β-咔啉酮,产率良好。克级实验和四氢-β-咔啉酮的进一步衍生化突出了我们方法的潜在应用价值。