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Piperidine → (R)-3-(4-Formylbenzoylamino)-2-hydroxypropionic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Piperidine | HCID 8082 | — |
| 反応物 | 4-Formylbenzoic acid | HCID 12088 | — |
| 反応物 | Diisopropylcarbodiimide | HCID 12734 | — |
| 反応物 | 1-Hydroxybenzotriazole | HCID 75771 | — |
| 反応物 | (R)-Fmoc-isoserine | HCID 7408673 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 溶媒 | N-methyl-2-pyrrolidone | HCID 13387 | — |
| 生成物 | (R)-3-(4-Formylbenzoylamino)-2-hydroxypropionic acid | HCID 86586064 | — |
反応手順
To the above resin bound (R)-Fmoc-isoserine was added 500 μL of a 20% solution of piperidine in DMF. Upon shaking for 30 min, the resin was drained and washed with N-methyl-2-pyrrolidinone (6×1 mL). Then, 200 μmol 4-formylbenzoic acid (30 mg) and 200 μmol HOBt (31 mg) was dissolved in N-methyl-2-pyrrolidinone (500 μL) and added to the resin followed by 200 μmol diisopropyl carbodiimide (25.2 mg) dissolved in acetonitrile (500 μL). The mixture was shaken for 4 hours at 25° C. followed by filtration and washing of the resin with N-methyl-2-pyrrolidinone (3×1 mL).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06562807B2 |
| 出典データセット | uspto-grants-2003_05 |
| ORD ID | ord-fe41ed78558740f381eb97a1989fd813 |
| 出典メモ | uspto-grants-2003_05 |