化工社化工社 化学情報印刷レポート · 研究参考用
Pyridine → [1-(3,5-Difluoro-phenyl)-5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]-(4,4-difluoro-piperidin-1-yl)-methanone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Pyridine | HCID 1049 | — |
| 反応物 | (3,5-Difluorophenyl)boronic acid | HCID 2734338 | — |
| 反応物 | (4,4-Difluoropiperidin-1-yl)[5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]methanone | HCID 11603838 | — |
| 触媒 | Cupric acetate | HCID 8895 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | [1-(3,5-Difluoro-phenyl)-5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]-(4,4-difluoro-piperidin-1-yl)-methanone | HCID 16739413 | — |
反応手順
A mixture of (4,4-difluoro-piperidin-1-yl)-[5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]-methanone (intermediate 1, 100 mg, 1.0 eq.), anhydrous copper(II) acetate (90 mg, 2.0 eq.), 3,5-difluorophenylboronic acid (123 mg, 3 eq.) and pyridine (80 uL, 4 eq.) in dichloromethane (2.5 mL) was stirred at room temperature for 2 days, evaporated to dryness and purified on silica gel, eluting with a 98:2 to 95:5 gradient of dichloromethane/methanol, to yield 79 mg (61%) from the desired product as light yellow foam. MS (m/e): 518.4 (MH+, 100%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07745479B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-d70fcd0359ab47f8b28dc0012ec92a30 |
| 出典メモ | uspto-grants-2010_06 |