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Water → 2-butyl-5-((4-(trifluoromethyl)pyridin-3-yl)methylamino)isoindolin-1-one TFA
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | 4-(Trifluoromethyl)pyridine-3-carbaldehyde | HCID 21354724 | — |
| 反応物 | 5-Amino-2-butyl-2,3-dihydro-1H-isoindol-1-one | HCID 67432065 | — |
| 触媒 | Zincchloride | HCID 3007855 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | 2-butyl-5-((4-(trifluoromethyl)pyridin-3-yl)methylamino)isoindolin-1-one TFA | HCID 86762286 | 19% |
反応手順
5-amino-2-butylisoindolin-1-one (35.0 mg, 0.17 mmol), ZnCl2 (14.0 mg, 0.10 mmol) and NaCNBH4 (12.9 mg, 0.21 mmol) were consecutively added to a solution of 4-(trifluoromethyl)nicotinaldehyde (30.0 mg, 0.17 mmol) in MeOH (4 mL). After stirring overnight at room temperature excess water was added. The reaction mixture was extracted with EtOAc, the combined org. layers were washed with water, dried (MgSO4) and the solvent was removed in vacuo. Purification by HPLC provided 2-butyl-5-((4-(trifluoromethyl)pyridin-3-yl)methylamino)isoindolin-1-one TFA (16.0 mg, 19%). ESI-MS [M+H]+=364.2.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08664214B2 |
| 出典データセット | uspto-grants-2014_03 |
| ORD ID | ord-dafe9df8dd884e4aae5de41dfe250f89 |
| 出典メモ | uspto-grants-2014_03 |