化工社化工社 化学情報印刷レポート · 研究参考用
Triethylamine → N-(1,1-dimethyl-2-morpholin-4-ylethyl)-2-{5-(4-fluorobenzyl)-3-[1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl]-1H-pyrazol-1-yl}acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 2-Methyl-1-(morpholin-4-yl)propan-2-amine | HCID 201497 | — |
| 反応物 | Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 9886157 | — |
| 反応物 | {5-(4-fluorobenzyl)-3-[1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl]-1H-pyrazol-1-yl}acetic acid | HCID 67092066 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | N-(1,1-dimethyl-2-morpholin-4-ylethyl)-2-{5-(4-fluorobenzyl)-3-[1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl]-1H-pyrazol-1-yl}acetamide | HCID 67091944 | 97.7% |
反応手順
A mixture of {5-(4-fluorobenzyl)-3-[1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl]-1H-pyrazol-1-yl}acetic acid (1.0 g, 2.37 mmol), 1,1-dimethyl-2-morpholin-4-yl-ethylamine (0.375 g, 2.37 mmol), HATU (0.71 g, 2.85 mmol) and Et3N (0.71 g, 7.1 mol) in DMF (20 mL) was stirred at room temperature overnight. The mixture was concentrated in vacuo and the residue was treated with water (50 mL) and CH2Cl2 (50 mL). The aqueous layer was extracted with CH2Cl2 (2×20 mL). The combined organics were dried over Na2SO4 and evaporated to afford crude title compound (1.3 g, 92%) as yellow oil that was used without further purification in next step.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07919488B2 |
| 出典データセット | uspto-grants-2011_04 |
| ORD ID | ord-c10ded2ac5914199a5d6b33f2d6c83ee |
| 出典メモ | uspto-grants-2011_04 |