Key Laboratory of Functional Small Organic Molecules, Ministry of Education and Jiangxi Key Laboratory of Green Chemistry, College of Chemistry & Chemical Engineering, Jiangxi Normal University, Nanchang, Jiangxi 330022, P. R. China.
Org Biomol Chem. 2021 Apr 26;19(15):3359-3369. doi: 10.1039/d1ob00128k.
Various β-indolyl sulfoximidoyl amides were efficiently prepared from ortho-iodoanilines, propargyl bromides, 1 atm of CO, and substituted NH-sulfoximines, through a palladium-catalyzed indole annulation/carbonyl insertion/C-N bond formation cascade. Mostly good to high yields of the products were obtained through this multi-step, one-pot reaction protocol under very gentle reaction conditions. The obtained β-indolyl sulfoximidoyl amides could be converted into biologically interesting sulfoximine analogues that contain a tryptamine moiety.
各种β-吲哚基磺酰亚胺酰胺可通过钯催化吲哚环化/羰基插入/C-N 键形成级联反应，从邻碘苯胺、丙炔溴、1 大气压 CO 和取代的 NH-磺酰亚胺胺高效制备。通过这种多步、一锅反应方案，在非常温和的反应条件下，得到的产物产率大多为好到高。得到的β-吲哚基磺酰亚胺酰胺可转化为含有色胺部分的生物感兴趣的磺酰胺类似物。
