With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.387-43-9,4-Fluoroindole,as a common compound, the synthetic route is as follows.
To a solution of 4-fluoro-lH-indole (150 g, l . l lmol) and DMAP (4.5 g, 3percentWt) in THF (2.5 L) was added (Boc)20 (255 g, 1.16 mol) dropwise. The mixture was stirred at room temperature overnight. The organic solvent was removed in vacuum, and the residue was purified by column chromatography (PE) to give tert-butyl 4-fluoro-lH-indole-l-carboxylate (250 g, yield: 96percent). 1H- MR (CDC13, 400 MHz) delta 7.92 (d, J= 8.4 Hz, 1H), 7.55 (d, J= 3.6 Hz, 1H), 7.23 (m, 1H), 6.90 (m, 1H), 6.66 (d, J = 3.6 Hz, 1H), 1.67 (s, 9H). MS (M+H)+: 236.
387-43-9, 387-43-9 4-Fluoroindole 2774502, aindole-building-block compound, is more and more widely used in various fields.
Reference£º
Patent; MERCK SHARP & DOHME CORP.; HE, Shuwen; DAI, Xing; PALANI, Anandan; NARGUND, Ravi; LAI, Zhong; ZORN, Nicolas; XIAO, Dong; DANG, Qun; LI, Peng; PENG, Xuanjia; SOLL, Richard; WO2014/121418; (2014); A1;,
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