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Bromine → 5-(5-Bromo-2-(4-fluorophenyl)thiazol-4-yl)-3-methoxypyridin-2-amine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Bromine | HCID 24408 | — |
| 反応物 | 5-(2-(4-Fluorophenyl)thiazol-4-yl)-3-methoxypyridin-2-amine | HCID 66590954 | — |
| 溶媒 | Chloroform | HCID 6212 | — |
| 生成物 | 5-(5-Bromo-2-(4-fluorophenyl)thiazol-4-yl)-3-methoxypyridin-2-amine | HCID 66591192 | 76.6% |
反応手順
To a solution of 5-(2-(4-fluorophenyl)thiazol-4-yl)-3-methoxypyridin-2-amine (68 mg, 0.23 mmol) in chloroform (3.6 mL) at 0° C. was added a solution of bromine (2.0 M in CHCl3, 0.17 mL, 0.34 mmol). The reaction was stirred at rt for 6-10 min and concentrated in vacuo. The resulting residue was azeotroped with 5% methanol in DCM solution (5 mL) and purified by prep TLC (SiO2, 1.0 mm, 95:5 DCM-methanol) to give 67 mg of 5-(5-bromo-2-(4-fluorophenyl)thiazol-4-yl)-3-methoxypyridin-2-amine was isolated as a tan solid: LCMS (m/z): 380.0 (MH+), tR=0.85 min.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08865732B2 |
| 出典データセット | uspto-grants-2014_10 |
| ORD ID | ord-7813d0220a3a4d9d888f8259d1937c63 |
| 出典メモ | uspto-grants-2014_10 |