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A concise silylamine approach to 2-amino-3-hydroxy-indoles with potent in vivo antimalaria activity.
| Publication Type | Journal Article |
| Authors | Urgaonkar, S., Cortese JF, Barker RH, Cromwell M., Serrano AE, Wirth DF, Clardy J., and Mazitschek R. |
| 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. |
| Year of Publication | 2010 |
| Journal | Organic letters |
| Volume | 12 |
| Issue | 18 |
| Pages | 3998-4001 |
| Date Published (YYYY/MM/DD) | 2010/09/17 |
| ISSN Number | 1523-7060 |
| DOI | 10.1021/ol101566h |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/20718474?dopt=Abstract |
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