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N-(2-Aminoethyl)isoquinoline-5-sulfonamide → Isoquinoline-5-sulfonic acid {2-[2-(4-bromo-2-isoxazol-5-yl-phenoxy)-ethylamino]-ethyl}-amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | N-(2-Aminoethyl)isoquinoline-5-sulfonamide | HCID 3544 | — |
| 反応物 | Diisobutylaluminum hydride | HCID 14487 | — |
| 反応物 | (4-Bromo-2-isoxazol-5-yl-phenoxy)-acetic acid methyl ester | HCID 69277354 | — |
| 生成物 | Isoquinoline-5-sulfonic acid {2-[2-(4-bromo-2-isoxazol-5-yl-phenoxy)-ethylamino]-ethyl}-amide | HCID 58816135 | — |
反応手順
By following a similar procedure as described in Example 34, DIBAL-H reduction of (4-bromo-2-isoxazol-5-yl-phenoxy)-acetic acid methyl ester, and subsequent reductive amination with isoquinoline-5-sulfonic acid (2-amino-ethyl)-amide gives the free amine of the title compound as a white solid. ESIMS: m/z 517 [(M+H)+, 79Br], 519 [(M+H)+, 81Br].
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07414063B2 |
| 出典データセット | uspto-grants-2008_08 |
| ORD ID | ord-5f8380b4ed044931a993709dd4f142d0 |
| 出典メモ | uspto-grants-2008_08 |