反式-2,3-二取代吲哚啉衍生物的不对称合成。
Asymmetric synthesis of trans-2,3-disubstituted indoline derivatives.
机构信息
Department of Chemistry, Konkuk University, Seoul 143-701, Korea.
出版信息
J Org Chem. 2012 Jan 6;77(1):808-12. doi: 10.1021/jo2023526. Epub 2011 Dec 19.
PMID:22148595
Abstract
A novel method for asymmetric synthesis of trans-2,3-disubstituted indolines has been developed. The strategy involves the (-)-sparteine-mediated electrophilic substitution of 2-benzyl N-pivaloylaniline with aromatic or α,β-unsaturated aldehydes and subsequent intramolecular nucleophilic substitution. The simple protocol for two-step process can produce highly enantioenriched indolines 3a-o up to 98:2 er.
摘要
已开发出一种用于反式-2,3-二取代吲哚啉不对称合成的新方法。该策略涉及 (-)-胡椒碱介导的 2-苄基 N-特戊酰苯胺与芳族或α,β-不饱和醛的亲电取代，以及随后的分子内亲核取代。两步法的简单方案可以高产率（高达 98:2 er）得到高度对映富集的吲哚啉 3a-o。
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