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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|
|Date Published (YYYY/MM/DD)||2010/09/17|