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Benzenesulfonamide → 3-{(5-oxo-1-(3-{(benzylamino)carbonylamino}phenyl)pyrrolidin-3-yl)carbonylamino}-N-(phenylsulfonyl)-3-(3-pyridyl)propanamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Benzenesulfonamide | HCID 7370 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | 3-{(5-Oxo-1-(3-{(benzylamino)carbonylamino}phenyl)pyrrolidin-3-yl)carbonylamino}-3-(3-pyridyl)propanoic acid | HCID 22591800 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 3-{(5-oxo-1-(3-{(benzylamino)carbonylamino}phenyl)pyrrolidin-3-yl)carbonylamino}-N-(phenylsulfonyl)-3-(3-pyridyl)propanamide | HCID 12135087 | — |
反応手順
A suspension of 3-{(5-oxo-1-(3-{(benzylamino)carbonylamino}phenyl)pyrrolidin-3-yl)carbonylamino}-3-(3-pyridyl)propanoic acid (60 mg, 0.11 mmol), benzenesulfonamide (Aldrich, 18 mg, 0.11 mmol), 1-ethyl-3-(3-(dimethylamino)propyl)carbodiimide hydrochloride (22 mg, 0.11 mmol), and dimethyl-4-pyridylamine (Aldrich, 0.22 mmol) in CH2Cl2 (5 mL) was stirred at room temperature for 2 days. A white solid was filtered and further purified by preparative HPLC. The title compound was obtained as a white solid. MS (ES+): 643 (M+H)+; (ES−): 641 (M−H)−.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06849639B2 |
| 出典データセット | uspto-grants-2005_02 |
| ORD ID | ord-64de064dac864013aed39b5a4115ee3d |
| 出典メモ | uspto-grants-2005_02 |