Valles Daniel A, Dutta Subhradeep, Paul Anirudra, Abboud Khalil A, Ghiviriga Ion, Seidel Daniel
Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, Florida 32611, United States.
Center for X-ray Crystallography, Department of Chemistry, University of Florida, Gainesville, Florida 32611, United States.
Org Lett. 2021 Aug 20;23(16):6367-6371. doi: 10.1021/acs.orglett.1c02187. Epub 2021 Jul 29.
A simple one-pot procedure enables the sequential, regioselective, and diastereoselective introduction of the same or two different substituents to the α- and α'-positions of unprotected azacycles. Aryl, alkyl, and alkenyl substituents are introduced via their corresponding organolithium compounds. The scope of this transformation includes pyrrolidines, piperidines, azepanes, and piperazines.
一种简单的一锅法程序能够将相同或两个不同的取代基顺序、区域选择性和非对映选择性地引入到未保护氮杂环的α-和α'-位。芳基、烷基和烯基取代基通过它们相应的有机锂化合物引入。这种转化的范围包括吡咯烷、哌啶、氮杂环庚烷和哌嗪。
