EaStCHEM, School of Chemistry, University of St. Andrews, North Haugh, St. Andrews KY16 9ST, UK.
Org Lett. 2013 Jul 5;15(13):3472-5. doi: 10.1021/ol401554y. Epub 2013 Jun 25.
Telescoped and one-pot olefination/asymmetric functionalization approaches to disubstituted pyrrolidines (dr up to 99:1, up to 99% ee) have been developed using commercially available tetramisole (0.1 to 5 mol %). Using OTMS-quinidine as the Lewis base gives preferential access to an anti-configured pyrrolidine in high enantioselectivity.
已开发出使用商业可得的四咪唑(0.1 至 5 摩尔%)进行二取代吡咯烷的缩合和一锅法烯烃化/不对称官能化方法(dr 高达 99:1,ee 高达 99%)。使用 OTMS-奎宁作为路易斯碱可以优先得到高对映选择性的反式构型吡咯烷。