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Organic letters DOI:10.1021/ol101566h

A concise silylamine approach to 2-amino-3-hydroxy-indoles with potent in vivo antimalaria activity.

Publication TypeJournal Article
Year of Publication2010
AuthorsUrgaonkar, S, Cortese, JF, Barker, RH, Cromwell, M, Serrano, AE, Wirth, DF, Clardy, J, Mazitschek, R
JournalOrganic letters
Volume12
Issue18
Pages3998-4001
Date Published2010/09/17
ISSN1523-7060
Abstract

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.

URLhttp://dx.doi.org/10.1021/ol101566h
DOI10.1021/ol101566h
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/20718474?dopt=Abstract