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Diisopropylethylamine → 4-{3-[5-(3-Fluoro-4-methanesulfonyl-phenyl)-4-methyl-thiazol-2-yl]-ureido)-butyric acid ethyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | Ethyl 4-isocyanatobutyrate | HCID 3445674 | — |
| 反応物 | 5-(3-Fluoro-4-(methylsulfonyl)phenyl)-4-methylthiazol-2-amine | HCID 57351277 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 4-{3-[5-(3-Fluoro-4-methanesulfonyl-phenyl)-4-methyl-thiazol-2-yl]-ureido)-butyric acid ethyl ester | HCID 86598431 | — |
反応手順
5-(3-Fluoro-4-methanesulfonyl-phenyl)-4-methyl-thiazol-2-ylamine (Example 72), (0.1 g, 0.31 mmol) DIPEA (0.039 ml, 0.34 mmol), ethyl-4-isocyanatobutyrate (0.046 ml, 0.31 mmol) in DCM (2 ml) are heated together at reflux overnight. The reaction mixture is diluted with DCM (20 ml) and washed with 1M hydrochloric acid (15 ml), water (2×15 ml), brine (15 ml), dried over MgSO4, filtered and concentrated in vacuo to yield the titled compound as an off white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07687637B2 |
| 出典データセット | uspto-grants-2010_03 |
| ORD ID | ord-704a95a01a334b7eb2d6fbfa17200dbb |
| 出典メモ | uspto-grants-2010_03 |