吡咯烷酮衍生物的直接胺化: 构建偕二胺衍生物

doi:10.6023/cjoc201410017

摘要/Abstract

研究了对甲苯磺酸(PTSA)催化的吡咯烷酮化合物与各种N-亲核试剂的胺化反应. 该方法通过简单抽滤就能以中等至优良产率得到一系列的偕二胺化合物, 后处理简单无需柱层析, 且可以将反应放大至克级规模.

A novel 4-methylbenzenesulfonic acid (PTSA)-catalyzed intermolecular amination of N-acyliminium species with various N-sources via benzylic C(sp³)-O activation of functionalized 2-oxo-1-pyrrolidine derivatives has been developed. This method provides an efficient and chromatography-free access to gem-diamines equivalent with moderate to good yields. Because of the importance of gem-diamine derivatives, the methodology is expected to have a significant value for practical applications.

Key words: N-acyliminium ion, gem-diamines, green chemistry

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杨锦明, 褚雪强, 纪顺俊. 吡咯烷酮衍生物的直接胺化: 构建偕二胺衍生物[J]. 有机化学, 2014, 34(12): 2462-2470.

Yang Jinming, Chu Xueqiang, Ji Shunjun. Direct Amination of N-Acyliminium Ion Surrogates: A Convenient Access to gem-Diamines Derivatives[J]. Chin. J. Org. Chem., 2014, 34(12): 2462-2470.

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