化工社化工社 化学情報印刷レポート · 研究参考用
Sodium Chloride → Trandolapril
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sodium Chloride | HCID 5234 | — |
| 反応物 | Methanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 2733084 | — |
| 反応物 | (2S,3aR,7aS)-octahydro-1H-indole-2-carboxylic acid | HCID 7018901 | — |
| 反応物 | N-(1-ethoxycarbonyl-3-phenylpropyl)-L-alanine | HCID 13044262 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 溶媒 | Triethylamine | HCID 8471 | — |
| 生成物 | Trandolapril | HCID 5484727 | 92% |
反応手順
To 2.79 g of (S)-1-(N-(1-(ethoxycarbonyl)-3-phenylpropyl)-L-alanine and 1.75 g of (2S,3aR,7aS)-octahydro-1H-indol-2-carboxylic acid in 100 ml of acetonitrile and 5 ml DMF first 2.9 ml of triethylamine and then with stirring 3.8 g O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate were and the stirring of the mixture was continued for 30 minutes at room temperature. Finally, 300 ml of saturated NaCl solution was added and the mixture was extracted twice with 100 ml of ethyl acetate. After isolation of the product, which was done by the same way as in example 1, 3.96 g (92%) of trandolapril was obtained.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07671215B2 |
| 出典データセット | uspto-grants-2010_03 |
| ORD ID | ord-ea87d675a8b64bf4ac30b3d92c8d90c9 |
| 出典メモ | uspto-grants-2010_03 |