Hydrochloric Acid → 1-(4-Bromophenyl)cyclopropanamine
反応式
[Br:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2([NH:11]C(=O)OC(C)(C)C)[CH2:10][CH2:9]2)=[CH:4][CH:3]=1.Cl>CO.C1COCC1>[Br:1][C:2]1[CH:3]=[CH:4][C:5]([C:8]2([NH2:11])[CH2:9][CH2:10]2)=[CH:6][CH:7]=1参加物
5
反応条件
- 温度
- 35 °C
実験手順
To a solution of tert-butyl [1-(4-bromophenyl)-cyclopropyl]-carbamate (Intermediate 115, 1.08 g, 3.40 mmols) in 20 mL MeOH and 20 mL THF was added 20 mL of 3M aqueous HCl. The solution was warmed to 35° C. for 3 hours and then stirred for 17 h at 25° C. The reaction was quenched by adjusting the pH of the solution to 12 with 3M aqueous NaOH. The mixture was extracted with Et2O and the combined organic layers were washed with H2O and saturated aqueous NaCl before being dried (MgSO4) and concentrated under reduced pressure. The title compound 613 mg (85%) was used without further purification.
後処理
- customThe reaction was quenched
- extractionThe mixture was extracted with Et2O
- washthe combined organic layers were washed with H2O and saturated aqueous NaCl
- dry with materialbefore being dried (MgSO4)
- concentrationconcentrated under reduced pressure
- customThe title compound 613 mg (85%) was used without further purification
出典と根拠
- ORDレコード
- ord-45d832dfa241442bbc83a81f36563672
- 出典データセット
- uspto-grants-2005_02
- 特許番号
- US06855512B2
反応ノート
読み込み中…