Infectious Disease Initiative Program, The Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, Massachusetts 02142, USA.
Org Lett. 2010 Sep 17;12(18):3998-4001. doi: 10.1021/ol101566h.
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.
本文报道了一种简洁的策略来合成 2-氨基-3-羟基吲哚，这些化合物被揭示为具有强效体内活性的新型抗疟药物。以色胺酮为起始原料，通过使用叔丁基二甲基硅基胺（TBDMSNH（2））作为以前未探索的氨等价物，经氧吲哚中间体两步反应以良好的收率合成目标化合物。
