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Dimethylformamide → 2-{3-Pyridin-3-yl-1-[(5-pyridin-2-yl-2-thienyl)carbonyl]-4,5-dihydro-1h-pyrazol-5-yl}phenol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dimethylformamide | HCID 6228 | — |
| 反応物 | 1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide | HCID 15908 | — |
| 反応物 | 3-(Pyridin-2-yl)thiophene-2-carboxylic acid | HCID 10242043 | — |
| 反応物 | 2-(3-pyridin-3-yl-4,5-dihydro-1H-pyrazol-5-yl)phenol | HCID 22696396 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | 2-{3-Pyridin-3-yl-1-[(5-pyridin-2-yl-2-thienyl)carbonyl]-4,5-dihydro-1h-pyrazol-5-yl}phenol | HCID 24963588 | 49% |
反応手順
To a solution of 2-(3-pyridin-3-yl-4,5-dihydro-1H-pyrazol-5-yl)phenol (600 mg, 2.51 mmol) and pyridine-2-ylthiophene-2-carboxylic acid (515 mg, 2.51 mmol) in DCM (10 mL) was added EDCI (580 mg, 3.00 mmol) and DMF (3 mL). After stirring for 12 h, water and EtOAc were added. The resulting solid was filtered and washed with EtOAc and cold MeOH and dried under vacuum to give 2-[3-pyridin-3-yl-1-[(5-pyridin-2-yl-2-thienyl)carbonyl]-4,5-dihydro-1H-pyrazol-5-yl]phenol (I-76) (520 mg, 49%). LCMS: (AA) ES+ 427.4.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07795249B2 |
| 出典データセット | uspto-grants-2010_09 |
| ORD ID | ord-8f7cf0907c69431991e4513c4b93f966 |
| 出典メモ | uspto-grants-2010_09 |