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Sodium Carbonate → 7-[3-(2-Methyl-2H-[1,2,3]triazol-4-yl)phenyl]-3-trifluoromethylimidazo[1,2-b][1,2,4]triazine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sodium Carbonate | HCID 10340 | — |
| 反応物 | 7-Bromo-3-trifluoromethyl-imidazo[1,2-B][1,2,4]triazine | HCID 11601416 | — |
| 反応物 | HCID 22329492 | HCID 22329492 | — |
| 触媒 | HCID 178418397 | HCID 178418397 | — |
| 溶媒 | 1,2-Dimethoxyethane | HCID 8071 | — |
| 生成物 | 7-[3-(2-Methyl-2H-[1,2,3]triazol-4-yl)phenyl]-3-trifluoromethylimidazo[1,2-b][1,2,4]triazine | HCID 10154590 | 34% |
反応手順
This reaction was carried out as described in Example 37, step e, using 4-[3-(5,5-dimethyl-[1,3,2]dioxaborinan-2-yl)phenyl]-2-methyl-2H-[1,2,3]triazole (190 mg, 0.7 mmol), 7-bromo-3-trifluoromethylimidazo[1,2-b][1,2,4]triazine (0.156 g, 0.585 mmol), 2 M Na2CO3 (0.70 ml) and tetrakis(triphenylphosphine)palladium(0) (0.034 g) in 1,2-dimethoxyethane (2 ml). The crude residue was purified by flash chromatography (silica gel, 50% Et2O/toluene) and crystallized from toluene to yield the title compound (68 mg, 34%): 1H NMR (400 MHz, CDCl3) δ 4.28 (3H, s), 7.63 (1H, t, J 7.8 Hz), 7.87 (1H, dt, J 7.8, 1.4 Hz), 7.91 (1H, s), 8.05-8.09 (1H, m), 8.52 (1H, t, J 1.4 Hz), 8.68 (1H, s), 8.85 (1H, s); MS (ES+) m/z 346 [M+H]+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06936608B2 |
| 出典データセット | uspto-grants-2005_08 |
| ORD ID | ord-c3f4d7c0b39c4c82b5a97ff5cfa42e8a |
| 出典メモ | uspto-grants-2005_08 |