Scientific Publications

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

Publication TypeJournal Article
AuthorsUrgaonkar, S., Cortese JF, Barker RH, Cromwell M., Serrano AE, Wirth DF, Clardy J., and Mazitschek R.
AbstractThe 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.
Year of Publication2010
JournalOrganic letters
Volume12
Issue18
Pages3998-4001
Date Published (YYYY/MM/DD)2010/09/17
ISSN Number1523-7060
DOI10.1021/ol101566h
PubMedhttp://www.ncbi.nlm.nih.gov/pubmed/20718474?dopt=Abstract