Green Catalysis Center and College of Chemistry, Zhengzhou University, Zhengzhou, Henan Province 450001, People's Republic of China.
Org Lett. 2021 Dec 17;23(24):9625-9630. doi: 10.1021/acs.orglett.1c03859. Epub 2021 Nov 30.
The annulation of -cyclopropyl enamines to produce 1,4-dihydropyridine (1,4-DHP) derivatives is described. In the presence of molecular iodine (I), an -cyclopropyl enamine substrate undergoes iodination, opening of the cyclopropyl ring, and annulation with a second molecule of the substrate to form the 1,4-DHP product. This reaction is amenable to gram-scale operations under mild reaction conditions with no transition metals being required. Further transformations of the 1,4-DHPs leads to related pyridine and bicyclic frameworks.
描述了 -环丙基烯胺环化生成 1,4-二氢吡啶 (1,4-DHP) 衍生物的反应。在分子碘 (I) 的存在下，-环丙基烯胺底物发生碘化、开环以及与第二个底物分子的环化反应，形成 1,4-DHP 产物。该反应在温和的反应条件下可适用于克级规模操作，无需使用过渡金属。进一步对 1,4-DHPs 进行转化可得到相关的吡啶和双环骨架。
