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Dichloromethane → (2R)-2-(4-Chlorobenzenesulfonylamino)-4-methylpentanoic acid amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dichloromethane | HCID 6344 | — |
| 反応物 | 4-Chlorobenzenesulfonyl chloride | HCID 7398 | — |
| 反応物 | (R)-2-Amino-4-methylpentanamide | HCID 7271815 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | (2R)-2-(4-Chlorobenzenesulfonylamino)-4-methylpentanoic acid amide | HCID 59001058 | — |
反応手順
The above polymer-bound D-Leu-NH2 (20 g) was treated with CH2Cl2 (150 mL), pyridine (100 mL) and 4-chlorophenylsulfonyl chloride (20.0 g, 94.8 mmol). The mixture was shaken for 24 h, drained, washed with DMF (4×200 mL), CH2Cl2 (4×200 mL) and concentrated to give polymer-bound (R)-2-(4-chlorobenzenesulfonylamino)-4-methylpentanoic acid amide as a yellow resin (22 g). The completion of the reaction and the loading of the resin (0.57 mmol/g) were determined by the treatment of 50 mg of the resin with 10% (v/v) TFA/CH2Cl2 (2 mL) to give 8.7 mg of (R)-2-(4-chlorobenzenesulfonylamino)-4-methylpentanoic acid amide.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07786122B2 |
| 出典データセット | uspto-grants-2010_08 |
| ORD ID | ord-466db7542208430f8cdf772885ad7a2d |
| 出典メモ | uspto-grants-2010_08 |