A Concise Silylamine Approach to 2-Amino-3-hydroxy-indoles with Potent in vivo Antimalaria Activity

作者:Urgaonkar Sameer; Cortese Joseph F; Barker Robert H; Cromwell Mandy; Serrano Adelfa E; Wirth Dyann F; Clardy Jon; Mazitschek Ralph*
来源:Organic Letters, 2010, 12(18): 3998-4001.
DOI:10.1021/ol101566h

摘要

The development of a concise strategy to access 2-amino-3-hydroxy-indoles, which are disclosed as novel antimalarials with potent in vivo activity, is reported. Starting from isatins the target compounds are synthesized in 2 steps and in good yields via oxoindole intermediates by employing tert-butyldimethylsilyl amine (TBDMSNH(2)) as previously unexplored ammonia equivalent.

  • 出版日期2010-9-17