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Potassium bisulfate → N-Cyclopropyl-4-fluoro-3-[2-(pyridin-2-ylamino)-thiazol-5-ylmethoxy]-benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium bisulfate | HCID 516920 | — |
| 反応物 | 3-hydroxy-4-fluoro-N-cyclopropylbenzamide | HCID 22019106 | — |
| 反応物 | (5-Chloromethylthiazol-2-yl)pyridin-2-ylamine hydrochloride | HCID 86591883 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | N-Cyclopropyl-4-fluoro-3-[2-(pyridin-2-ylamino)-thiazol-5-ylmethoxy]-benzamide | HCID 22019135 | 33% |
反応手順
To a suspension of NaR (16 mg, 60% in oil) in DMF (1 mL) was added a solution of 3-hydroxy-4-fluoro-N-cyclopropylbenzamide (58.5 mg, 0.3 mmol) in DMF (1 mL) at RT. After 10 min, (5-chloromethylthiazol-2-yl)pyridin-2-ylamine hydrochloride (Example 10A) (52.4 mg, 0.2 mmol) was added. The mixture was stirred at RT for 1 h and poured onto ice. The mixture was neutralized with 1 N KHSO4 solution and the precipitates were collected, washed with water and ethyl acetate to give the title compound as a light yellow solid (25.2 mg, 33%). MS m/z 385 (M+H)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07084160B2 |
| 出典データセット | uspto-grants-2006_08 |
| ORD ID | ord-87002b9f196d4b4bafaff983bc899b02 |
| 出典メモ | uspto-grants-2006_08 |