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Hydrochloric Acid → 5-({[(4-chloro-2,5-dimethylphenyl)sulfonyl](methyl)amino}methyl)-N-{2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]ethyl}-N-methylfuran-3-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Hydrochloric Acid | HCID 313 | — |
| 反応物 | 1,1'-Carbonyldiimidazole | HCID 68263 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 5-({[(4-Chloro-2,5-dimethylphenyl)sulfonyl](methyl)amino}methyl)furan-3-carboxylic acid | HCID 58393029 | — |
| 反応物 | 2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-N-methylethanamine | HCID 67217191 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 5-({[(4-chloro-2,5-dimethylphenyl)sulfonyl](methyl)amino}methyl)-N-{2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]ethyl}-N-methylfuran-3-carboxamide | HCID 58393096 | — |
反応手順
5-({[(4-chloro-2,5-dimethylphenyl)sulfonyl](methyl)amino}methyl)furan-3-carboxylic acid (30 mg, 0.08 mmol) was dissolved in DMF (1 mL) and CDI (20 mg, 0.12 mmol) was added. The mixture was stirred until acid activation was complete. 2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-N-methylethanamine.HCl (19 mg, 0.08 mmol) and DIPEA (0.042 mL, 0.24 mmol) were sonicated in DMF (1 mL) for 15 min, 0.5 mL of activated acid solution was added to 0.25 mL of amine solution and the reaction was microwaved (120° C., 200 W) for 20 min, then 2×60 min. A portion of the reaction was concentrated and purified using prep method A.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08623859B2 |
| 出典データセット | uspto-grants-2014_01 |
| ORD ID | ord-4d14727ff2774839ac87213170d252f8 |
| 出典メモ | uspto-grants-2014_01 |