Department of Biophysical Chemistry, Graduate School of Pharmaceutical Sciences , Tohoku University , Aoba, Sendai 980-8578 , Japan.
Org Lett. 2019 Jul 19;21(14):5505-5508. doi: 10.1021/acs.orglett.9b01805. Epub 2019 Jul 2.
We report that the organic superbase -Bu-P4 efficiently catalyzes the amination of methoxy(hetero)arenes with amine nucleophiles such as aniline, indoline, and aminopyridine derivatives. This catalytic reaction is effective for the transformation of electron-deficient methoxyarenes possessing diverse functionalities (carbonyl, cyano, nitro, and halogen) as well as methoxyheteroarenes, including pyrazine, quinoline, isoquinoline, and pyridine derivatives. Intramolecular reactions provide six- and seven-membered ring cyclic amine products.
我们报告称,有机超强碱 -Bu-P4 能有效地催化甲氧基(杂)芳烃与胺亲核试剂(如苯胺、吲哚和氨基吡啶衍生物)的胺化反应。该催化反应对具有多种官能团(羰基、氰基、硝基和卤素)的缺电子甲氧基芳烃以及包括吡嗪、喹啉、异喹啉和吡啶衍生物在内的甲氧基杂芳烃的转化是有效的。分子内反应提供六元和七元环环状胺产物。