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3,5-Bis-trifluoromethylphenylboronic acid → 5-(3,5-Di(trifluoromethyl)phenyl)-3-(1-Methylpiperidin-4-yl)-4-Aza-1H-Indole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3,5-Bis-trifluoromethylphenylboronic acid | HCID 156265 | — |
| 反応物 | 5-Trifluoromethanesulfonyloxy-3-(1-methylpiperidin-4-yl)pyrrolo[3,2-b]pyridine | HCID 12041812 | — |
| 生成物 | 5-(3,5-Di(trifluoromethyl)phenyl)-3-(1-Methylpiperidin-4-yl)-4-Aza-1H-Indole | HCID 9867191 | 90.7% |
反応手順
O-Trifluoromethanesulfonyl-3-(1-methylpiperidin-4-yl)-5-hydroxy-4-aza-1H-indole (160 mg, 0.441 mmol) and 3,5-di(trifluoromethyl)phenylboronic acid (183 mg, 0.71 mmol) were converted to 171 mg of the title compound by the procedure of Example 3. (91%). MS(FD) m/e 427.6 (M+). EA calculated for C21H19F6N3: C, 59.02; H, 4.45; N, 9.84. Found: C, 59.31; H, 4.69; N, 9.83.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06358972B1 |
| 出典データセット | uspto-grants-2002_03 |
| ORD ID | ord-5c2a057212ee49f6aef2d3e848561246 |
| 出典メモ | uspto-grants-2002_03 |