Asymmetric Synthesis of trans-2,3-Disubstituted Indoline Derivatives

作者:Kang Kyoung Hee; Do Junghwan; Park Yong Sun*
来源:Journal of Organic Chemistry, 2012, 77(1): 808-812.
DOI:10.1021/jo2023526

摘要

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 alpha,beta-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.

  • 出版日期2012-1-6