三氟甲磺酸铜（Cu(OTf)）催化 -乙缩醛与异氰化物的 Ugi 型反应合成吡咯烷基和哌啶基 2-羧酰胺。
Cu(OTf) catalyzed Ugi-type reaction of ,-acetals with isocyanides for the synthesis of pyrrolidinyl and piperidinyl 2-carboxamides.
机构信息
School of Pharmacy and Institutes of Biomedical Sciences, Fudan University, 220 Handan Road, Shanghai, 200433, China.
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China.
出版信息
Chem Commun (Camb). 2021 Sep 14;57(73):9248-9251. doi: 10.1039/d1cc03113a.
The Cu(OTf) catalyzed Ugi-type reactions of ,-acetals with isocyanides have been described for the synthesis of pyrrolidinyl and piperidinyl 2-carboxamides. 4-Hydroxy-5-substituted-prolinamides can be obtained in high diastereoselectivities (2,4-/ > 19 : 1) and a stereoselective model was proposed for 2,4- selectivity. Moreover, 4-F-VH 032, a novel analog of the VHL ligand, was conveniently obtained by utilizing the present method.
Cu(OTf)催化的 -乙缩醛与异氰化物的 Ugi 型反应已被用于合成吡咯烷基和哌啶基 2-羧酰胺。4-羟基-5-取代脯氨酰胺可以以高非对映选择性（2,4-/ > 19 : 1）获得，并提出了 2,4-选择性的立体选择性模型。此外，通过利用本方法方便地获得了 VHL 配体的新型类似物 4-F-VH 032。
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