With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.128562-95-8,4-(Trifluoromethyl)-1H-indole,as a common compound, the synthetic route is as follows.
A. 1 -(2-Methoxy-ethyl)-4-trifluoromethyl-1 H-indole A mixture of 4-trifluoromethyl-1 H-indole (105 mg, 0.57 mmol), powder KOH (159 mg, 2.83 mmol) in DMSO (6 mL) is stirred at r.t. for 5 min. 2-Methoxyethyl bromide (80 muIota_, 0.85 mmol) is added. After the reaction mixture is stirred at r.t. overnight, it is partitioned between H2O and Et2O. The two layers are separated, and the aqueous layer is extracted with Et2O (3x). The combined organic extracts are washed with H2O and brine, dried over MgSO , filtered, and concentrated in vacuo. The crude material is purified on silica gel with heptane/EtOAc (100/0 to 70/30) as eluent to yield the product (100 mg, 72%) as a clear colorless liquid.1 H NMR (300 MHz, CDCI3) delta 7.53 (d, J = 8.2 Hz, 1 H), 7.40 (d, J = 7.3 Hz, 1 H), 7.35- 7.20 (m, 2H), 6.69 (s, 1 H), 4.32 (t, J = 5.4 Hz, 2H), 3.71 (t, J = 5.4 Hz, 2H), 3.31 (s, 3H);19F NMR (300 MHz, CDCI3) delta -60.99 (s, 3F);LC Rt: 3.21 min; MS 244 (M+H, 100%)., 128562-95-8
128562-95-8 4-(Trifluoromethyl)-1H-indole 19803703, aindole-building-block compound, is more and more widely used in various fields.
Reference£º
Patent; SANOFI; CHOI-SLEDESKI, Yong Mi; LIANG, Guyan; NIEDUZAK, Thaddeus R.; POLI, Gregory B.; SHUM, Patrick Wai-Kwok; STOKLOSA, Gregory T.; ZHAO, Zhicheng; WO2011/79102; (2011); A1;,
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