A Concise Silylamine Approach to 2-Amino-3-hydroxy-indoles with Potent in vivo Antimalaria Activity
| Autor: | Ralph Mazitschek, Mandy Cromwell, Adelfa E. Serrano, Robert H. Barker, Dyann F. Wirth, Joseph F. Cortese, Jon Clardy, Sameer Urgaonkar |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
Indoles
Molecular Structure Chemistry Plasmodium falciparum Organic Chemistry Silanes Biochemistry Article Antimalarials Mice Structure-Activity Relationship In vivo Animals Structure–activity relationship Molecule Organic chemistry Amine gas treating Amines Malaria Falciparum Physical and Theoretical Chemistry |
| Zdroj: | Org Lett |
| ISSN: | 1523-7052 1523-7060 |
| Popis: | [Image: see text] 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 (TBDMSNH2) as previously unexplored ammonia equivalent. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|