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1,2-Dichloroethane → N-(7-cyanomethyl-chroman-4-yl)-3-phenyl-3-(3-trifluoromethyl-benzenesulfonylamino)-propionamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1,2-Dichloroethane | HCID 11 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 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 | 3-Phenyl-3-(3-trifluoromethyl-benzenesulfonylamino)-propionic acid | HCID 45439091 | — |
| 反応物 | (4-Amino-chroman-7-yl)-acetonitrile | HCID 68929026 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-(7-cyanomethyl-chroman-4-yl)-3-phenyl-3-(3-trifluoromethyl-benzenesulfonylamino)-propionamide | HCID 68932619 | — |
反応手順
To a solution of (4-amino-chroman-7-yl)-acetonitrile (Step A, 400 mg, 2.15 mmol) in CH2Cl2 (15 mL) was added 3-phenyl-3-(3-trifluoromethyl-benzenesulfonylamino)-propionic acid (802 mg, 2.15 mmol), HATU (408 mg, 1.07 mmol), EDC (453 mg, 2.36 mmol), and DIEA (0.7 mL, 4.29 mmol). The resulting mixture was stirred at RT for 18 h. Solvent was evaporated in vacuo. The residue was purified by chromatography on silica gel. Elution with CH2Cl2:MeOH mixture (95:5) gave final compound. MS m/z: 544.12 (M+H). Calc'd. for C27H24F3N3O4S-543.56.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07425631B2 |
| 出典データセット | uspto-grants-2008_09 |
| ORD ID | ord-fbff2b1639764c1eba5441021395fb1d |
| 出典メモ | uspto-grants-2008_09 |