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Argatroban (USAN:INN:BAN:JAN) → Methyl 6-aminohexanoate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Argatroban (USAN:INN:BAN:JAN) | HCID 92721 | — |
| 反応物 | Methanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 2733084 | — |
| 反応物 | Methyl 12-aminododecanoate | HCID 3665980 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | Methyl 6-aminohexanoate | HCID 1810164 | 169.2% |
反応手順
To a solution of argatroban monohydrate (300 mg, 0.570 mmol) and methyl 12-aminododecanoate (compound YS-004-17) (132 mg, 0.576 mmol) in anhydrous DMF (15 mL) was added HBTU (258 mg, 0.680 mmol). Stirring was continued at room temperature for 16 hours. The precipitates formed during the reaction were filtered off and DMF was removed by vacuum distillation. The residue was purified by preparative TLC using solvents CH2Cl2 /MeOH/NH3 (90/10/1, v/v) to give the titled compound (140 mg) (Yield: 28%). 1HNMR (MeOH-4, 300 MHz).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05942620 |
| 出典データセット | uspto-grants-1999_08 |
| ORD ID | ord-ded843c5ff40426aae07ba2e7782ea1a |
| 出典メモ | uspto-grants-1999_08 |