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5-Pyridin-4-yl-thiophene-2-sulfonyl chloride → 5-Pyridin-4-yl-thiophene-2-sulfonic acid-[1-(1-chloro-isoquinolin-7-ylmethyl)-2-oxopyrrolidin-3-(s)-yl]-amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-Pyridin-4-yl-thiophene-2-sulfonyl chloride | HCID 10635045 | — |
| 反応物 | 3-(S)-Amino-1-(1-chloro-isoquinolin-7-ylmethyl)-pyrrolidin-2-one hydrochloride | HCID 20680708 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | 5-Pyridin-4-yl-thiophene-2-sulfonic acid-[1-(1-chloro-isoquinolin-7-ylmethyl)-2-oxopyrrolidin-3-(s)-yl]-amide | HCID 20680736 | — |
反応手順
5-Pyridin-4-yl-thiophene-2-sulfonyl chloride is added to a solution of 3-(S)-amino-1-(1-chloro-isoquinolin-7-ylmethyl)-pyrrolidin-2-one hydrochloride (0.12 g, 0.38 mmol) in pyridine (2 mL). The resulting mixture is stirred overnight then concentrated to dryness. The residue is diluted with methylene chloride and washed with saturated NaHCO3 solution and brine. The organic layer is dried over MgSO4, filtered and concentrated to give 105 mg of a crude solid. The crude product is purified by column chromatography eluting with 5% MeOH/CH2Cl2 to afford the title product (0.026 g, 0.052 mmol) as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06281227B1 |
| 出典データセット | uspto-grants-2001_08 |
| ORD ID | ord-61a4ae5177384a0aa1b856c2e173fc7c |
| 出典メモ | uspto-grants-2001_08 |