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2,3,5,6-Tetrafluorophenol → N-[(1-methyl-3-isobutyl-indole-2-cabonyl)leucinyl]-3-amino-4-oxo-5-(2,3,5,6-tetrafluorophenyloxy)-pentanoic acid, tert-butyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2,3,5,6-Tetrafluorophenol | HCID 69858 | — |
| 反応物 | Potassium Fluoride | HCID 522689 | — |
| 反応物 | Ethyl acetate hexane | HCID 21226206 | — |
| 反応物 | N-[(1-methyl-3-isobutyl-indole-2-cabonyl)leucinyl]-3-amino-5-bromo-4-oxo-pentanoic acid, tert-butyl ester | HCID 86756364 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | N-[(1-methyl-3-isobutyl-indole-2-cabonyl)leucinyl]-3-amino-4-oxo-5-(2,3,5,6-tetrafluorophenyloxy)-pentanoic acid, tert-butyl ester | HCID 86756363 | 72.4% |
反応手順
The titled product (47.6 mg, 72%, white solid) was prepared as described in Example 82 using the product of Example 88 (57.6 mg, 0.097 mmol), potassium fluoride (18.5 mg, 0.24 mmol), and 2,3,5,6-tetrafluorophenol (21.1 mg, 0.097 mmol) in DMF (2.0 ml). TLC (hexane/EtOAc, 50/50): Rf=0.55.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06184244B2 |
| 出典データセット | uspto-grants-2001_02 |
| ORD ID | ord-a522d2b1178044bea514733c1e72cef4 |
| 出典メモ | uspto-grants-2001_02 |