化工社化工社 化学情報印刷レポート · 研究参考用
1,2-Dichloroethane → (R)-tert-butyl 1-amino-3-(benzyloxy)-1-oxopropan-2-ylcarbamate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1,2-Dichloroethane | HCID 11 | — |
| 反応物 | Ammonium Hydroxide | HCID 14923 | — |
| 反応物 | (R)-3-(benzyloxy)-2-((tert-butoxycarbonyl)amino)propanoic acid | HCID 2733693 | — |
| 反応物 | 1-Hydroxybenzotriazole hydrate | HCID 2796029 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | (R)-tert-butyl 1-amino-3-(benzyloxy)-1-oxopropan-2-ylcarbamate | HCID 7216902 | 87.7% |
反応手順
To a solution of N-Boc-O-benzyl-D-serine (510 mg, 1.72 mmol) and HOBt hydrate (317 mg, 2.07 mmol) in DMF (9 mL), EDC (432 mg, 2.25 mmol) was added. The mixture was stirred for 60 min. Then conc. NH4OH (0.600 mL, ˜8.40 mmol) was added. It was stirred for 18 h. Water and EtOAc were added. The organic phase was separated, washed with 5% NaHCO3, dried over Na2SO4, concentrated in vacuo to give (R)-tert-butyl 1-amino-3-(benzyloxy)-1-oxopropan-2-ylcarbamate (444 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09359375B2 |
| 出典データセット | uspto-grants-2016_06 |
| ORD ID | ord-1003d443af964ada8ae07771af917bb3 |
| 出典メモ | uspto-grants-2016_06 |