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Citric Acid → Fmoc-L-aspartyl (t-butyl)-3-(aminomethyl)-benzoic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Citric Acid | HCID 311 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | Fmoc-L-aspartic acid | HCID 7019016 | — |
| 反応物 | 3-(Aminomethyl)benzoic acid hydrochloride | HCID 16218772 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | Fmoc-L-aspartyl (t-butyl)-3-(aminomethyl)-benzoic acid | HCID 131720031 | — |
反応手順
To a solution of FmocAsp (But) OPfp (17.33 g, 30 mmol) and the compound of Step 6 (6.19 g, 33 mmol) in 50 mL DMF cooled in an ice bath was added 11.5 mL (66 mmol) diisopropylethylamine, and after stirring at room temperature for 5 h, 200 mL 5% citric acid was added and the solution was extracted with ethyl acetate twice. The combined extracts were washed with brine, dried (MgSO4), and concentrated to give a solid which was washed with ether-petroleum ether and dried. Yield 16.3 g (100%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05635477 |
| 出典データセット | uspto-grants-1997_06 |
| ORD ID | ord-5fc4301d9d1d458cb627178a525b9f84 |
| 出典メモ | uspto-grants-1997_06 |