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2-Fluoropyridine → 1'-[(6-Chloro-1-pyridin-2-yl-1H-indol-3-yl)carbonyl]-3H-spiro[2-benzofuran-1,4'-piperidin]-3-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Fluoropyridine | HCID 9746 | — |
| 反応物 | Sodium hydride | HCID 24758 | — |
| 反応物 | 1'-[(6-chloro-1H-indol-3-yl)carbonyl]-3H-spiro[2-benzofuran-1,4'-piperidin]-3-one | HCID 59657599 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 1'-[(6-Chloro-1-pyridin-2-yl-1H-indol-3-yl)carbonyl]-3H-spiro[2-benzofuran-1,4'-piperidin]-3-one | HCID 59657622 | 38% |
反応手順
To a solution of 1′-[(6-chloro-1H-indol-3-yl)carbonyl]-3H-spiro[2-benzofuran-1,4′-piperidin]-3-one (prepared according to example 16 above) in dry DMF was added NaH (1 eq) and the reaction mixture stirred at room temperature for 30 min and then treated with 2-fluoropyridine (1.5 eq) and heated at 140° C. under microwave irradiation for 15 min. Purification by preparative HPLC gave the desired product in 38% yield.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07629353B2 |
| 出典データセット | uspto-grants-2009_12 |
| ORD ID | ord-3aaa92fa8181497a8e1a6fbfc7d7a13a |
| 出典メモ | uspto-grants-2009_12 |