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Potassium Carbonate → 1-Benzyl-N-(3,4-difluorobenzyl)-2-isopropyl-6-(1,3-thiazol-2-yloxy)-1H-indole-3-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | Sodium Hydroxide | HCID 14798 | — |
| 反応物 | 2-Bromothiazole | HCID 76430 | — |
| 反応物 | 1-Benzyl-N-(3,4-difluorobenzyl)-6-hydroxy-2-isopropyl-1H-indole-3-carboxamide | HCID 25160740 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | 1-Benzyl-N-(3,4-difluorobenzyl)-2-isopropyl-6-(1,3-thiazol-2-yloxy)-1H-indole-3-carboxamide | HCID 59762285 | — |
反応手順
General Procedure U. To a solution of 1-benzyl-N-(3,4-difluorobenzyl)-6-hydroxy-2-isopropyl-1H-indole-3-carboxamide (Compound 8, 12 mg, 0.028 mmol) in DMF (1 ml) was added K2CO3 (19 mg, 0.14 mmol) and 2-bromothiazole (23 mg, 0.14 mmol). The mixture was stirred at room temperature overnight and a small amount of NaOH was added. The reaction was kept stirring for 72 h, diluted with EtOAc, washed with brine, dried over Na2SO4, and concentrated in vacuo. The residue was purified by chromatography on silica gel (0→50% EtOAc-hexanes) to yield the title compound.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08524917B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-6316f0e3b36a47f98753bbe0910d7f24 |
| 出典メモ | uspto-grants-2013_09 |