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A diastereoselective three-component coupling approach to highly substituted pyrrolidines

机译:非对映选择性三组分偶联方法与高度取代的吡咯烷

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摘要

Building on the observation that metal complexation facilitates azomethine ylide formation, we report that chelating aldehydes participate in metal-templated, one-pot reactions with unprotected amino acid esters and activated olefins to provide highly substituted pyrrolidines. The high yields, broad substrate scope, excellent diastereoselectivities, functional group tolerance, and incorporation of commercially available materials in this reaction simplifies access to medicinally relevant proline derivatives.
机译:基于金属络合促进偶氮甲碱叶立德形成的观察,我们报道了螯合醛参与了金属模板化的一锅反应,与未保护的氨基酸酯和活化的烯烃形成高度取代的吡咯烷。高收率,广泛的底物范围,出色的非对映选择性,官能团耐受性以及在该反应中掺入可商购的材料,简化了获得医学上相关的脯氨酸衍生物的过程。

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