With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.166104-20-7,1-Boc-5-Aminoindole,as a common compound, the synthetic route is as follows.
To a stirred solution of tert-butyl 5-amino-1H-indole-1-carboxylate (1, 5.0 g, 21.55 mmol) in acetonitrile (50 mL) at 0 C., N-bromosuccinimide (4.23 g, 23.70 mmol) was added portion-wise. The mixture was stirred at same temperature for 3 h. Next, the reaction was poured into ice-cold water and extracted with ethyl acetate. The organic layer was washed with brine solution, dried over anhydrous sodium sulfate, filtered, and concentrated to dryness under reduced pressure. The crude product was purified by Combiflash (40 g, RediSep column) using 0-30% ethyl acetate in hexanes as eluent. The desired fractions were concentrated under reduced pressure to afford tert-butyl 5-amino-4-bromo-1H-indole-1-carboxylate (2) as a brown liquid. Yield: 5.8 g, 86%; MS (ESI) m/z 311.08 [M+1]+., 166104-20-7
166104-20-7 1-Boc-5-Aminoindole 11593831, aindole-building-block compound, is more and more widely used in various fields.
Reference£º
Patent; eFFECTOR Therapeutics, Inc.; ERNST, Justin T.; REICH, Siegfried H.; SPRENGELER, Paul A.; XIANG, Alan X.; (41 pag.)US2019/119256; (2019); A1;,
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