化工社化工社 化学情報印刷レポート · 研究参考用
Triethylamine → methyl (S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-4-[4-(6-hydroxy-2-oxo-1,4-dihydro-2H-quinazolin-3-yl)-piperidin-1-yl]-4-oxo-butanoate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Sodium Bicarbonate | HCID 516892 | — |
| 反応物 | O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate | HCID 2733207 | — |
| 反応物 | 6-Hydroxy-3-piperidin-4-yl-3,4-dihydro-1H-quinazolin-2-one | HCID 21102207 | — |
| 反応物 | 1-methyl (S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-succinate | HCID 86604295 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | methyl (S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-4-[4-(6-hydroxy-2-oxo-1,4-dihydro-2H-quinazolin-3-yl)-piperidin-1-yl]-4-oxo-butanoate | HCID 69071695 | — |
反応手順
A solution of 1.37 g (4.04 mmol) 1-methyl (S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-succinate, 1.42 g (4.40 mmol) TBTU, 0.63 mL (4.50 mmol) triethylamine and 1.00 g (4.04 mmol) 6-hydroxy-3-piperidin-4-yl-3,4-dihydro-1H-quinazolin-2-one in 10 mL DMF was stirred for 3 h at RT. The reaction mixture was poured onto 300 mL saturated NaHCO3 solution, the precipitated substance was suction filtered, washed with 50 mL water and dried at 60° C. in the circulating air dryer.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07696209B2 |
| 出典データセット | uspto-grants-2010_04 |
| ORD ID | ord-42f657904f034372909ef82d7e496329 |
| 出典メモ | uspto-grants-2010_04 |