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Sodium Thiosulfate → 2-amino-6-ethylsulfonyl-1H-benzoimidazole-4-carboxylic acid ethyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sodium Thiosulfate | HCID 24477 | — |
| 反応物 | m-Chloroperbenzoic acid | HCID 70297 | — |
| 反応物 | Sodium Bicarbonate | HCID 516892 | — |
| 反応物 | 2-amino-6-ethylsulfanyl-1H-benzoimidazole-4-carboxylic acid ethyl ester | HCID 66940818 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 2-amino-6-ethylsulfonyl-1H-benzoimidazole-4-carboxylic acid ethyl ester | HCID 66940531 | 94% |
反応手順
0.26 g (1.0 mmol) of 2-amino-6-ethylsulfanyl-1H-benzoimidazole-4-carboxylic acid ethyl ester (See Example 489) in DCM was stirred with 0.35 g (2.0 mmol) of MCPBA and 0.34 g (4.0 mmol) of NaHCO3 at room temperature for 3 h. The reaction mixture was treated with Na2S2O3 solution and stirred for 0.5 h at room temperature. EtOAc extraction, followed by washing with dilute NaOH solution and brine, and evaporation of the solvent produced 0.28 g (0.94 mmol, 94%) of 2-amino-6-ethylsulfonyl-1H-benzoimidazole-4-carboxylic acid ethyl ester. LCMS: 298 (M+1)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08946259B2 |
| 出典データセット | uspto-grants-2015_02 |
| ORD ID | ord-babaee2bcc8e45e395f7100dc6a09fdf |
| 出典メモ | uspto-grants-2015_02 |