関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 1-(6-Chloro-pyridine-3-sulfonyl)-4-methyl-piperazine | HCID 822457 | — |
| 反応物 | 2-Oxindole-6-carbonitrile | HCID 2773348 | — |
| 生成物 | Ammonia | HCID 222 | — |
| 生成物 | 2-Hydroxy-3-{5-[(4-methylpiperazin-1-yl)sulfonyl]pyridin-2-yl}-1H-indole-6-carbonitrile hydrochloride | HCID 136342135 | — |
反応手順
The title compound was prepared as described for Example 55 using 6-cyanooxindole (1.5 equ) and 1-(6-chloropyridine-3-sulfonyl)-4-methylpiperazine (1 equ; described in: Thunus L., Annales Pharmaceutiques Francaises 1977, 35, 197-203). Purification on a silica gel column using chloroform/methanol/conc. NH3(aq), (76:23: 1), as the eluent gave the title compound as the base. The base was dissolved in acetone/chloroform/methanol and treated with 5 M HCl in diethyl ether. The hydrochloride was dried to afford 24 mg (5.1% yield) of title compound: 1H NMR (DMSO-d6, 400 MHz) δ 14.87 (s, 1 H), 11.00 (s, 1 H), 10.21 (s, 1 H), 8.62 (s, 1 H), 7.83 (s, 2 H), 7.73 (d, J=8 Hz, 1 H), 7.38 (d, J=8 Hz, 1 H), 7.23 (s, 1 H), 3.81-3.67 (m, 2 H), 3.57-3.38 (m, 2 H), 3.22-3.05 (m, 2 H), 2.97-2.85 (m, 2 H), 2.77 (s, 3 H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US07399780B2 |
|---|
| 出典データセット | uspto-grants-2008_07 |
|---|
| ORD ID | ord-1081cd3652114fbf8793dd72dd579243 |
|---|
| 出典メモ | uspto-grants-2008_07 |
|---|
