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Ammonium Hydroxide → 2-(2-fluoro-5-((5-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)-1H-imidazol-2-yl)methyl)phenoxy)acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ammonium Hydroxide | HCID 14923 | — |
| 反応物 | methyl 2-(2-fluoro-5-((5-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)-1H-imidazol-2-yl)methyl)phenoxy)acetate | HCID 44546005 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | 2-(2-fluoro-5-((5-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)-1H-imidazol-2-yl)methyl)phenoxy)acetamide | HCID 44546069 | 86% |
反応手順
Methyl 2-(2-fluoro-5-((5-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)-1H-imidazol-2-yl)methyl)phenoxy)acetate (Example 93) (32.5 mg, 0.067 mmol) was treated with aqueous NH4OH (28-30%, 1 mL). The suspension was stirred at room temperature. After 2 hours, the reaction mixture was diluted with H2O (3 mL) and stirred for 30 min. The precipitate was filtered, washed with water, and dried under vacuum for overnight to afford the title compound (26.8 mg, 86%). (300 MHz, CDCl3) δ 2.49 (3H, s), 4.15 (2H, s), 4.51 (2H, s), 5.80 (N—H, 1H, bs), 6.71 (N—H, 1H, bs), 6.63-7.06 (4H, m), 7.25-7.28 (1H, m), 7.37-7.44 (2H, m), 7.94 (1H, dd), 8.10 (1H, d), 8.16-8.18 (2H, m), 8.91 (1H, dd), 11.00 (1H, bs). MS (ESI) m/z 468 (MH+).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08410146B2 |
| 出典データセット | uspto-grants-2013_04 |
| ORD ID | ord-1c87552265bd45babc5758d133ae2e6a |
| 出典メモ | uspto-grants-2013_04 |