関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline | HCID 45480181 | — |
| 反応物 | 8-Chloro-4-methyl-2-phenyl-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine | HCID 59577866 | — |
| 試薬 | Cesium carbonate | HCID 10796 | — |
| 触媒 | 2-(Dicyclohexylphosphino)biphenyl | HCID 2734216 | — |
| 触媒 | Palladium (II) acetate | HCID 4144353 | — |
| 溶媒 | 1,2-Dimethoxyethane | HCID 8071 | — |
| 生成物 | N-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)-4-methyl-2-phenyl-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepin-8-amine | HCID 49819935 | 37.23% |
反応手順
8-chloro-4-methyl-2-phenyl-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine (60.0 mg, 0.22 mmol), 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (57.7 mg, 0.28 mmol), palladium(II) acetate (4.90 mg, 0.02 mmol), 2-(Dicyclohexylphosphino)biphenyl (7.65 mg, 0.02 mmol) and CS2CO3 (213 mg, 0.66 mmol) were weighed into a microwave vial. The vial was capped and flushed with argon. DME (4 mL) was added and the mixture was heated to 100°C in a microwave apparatus for 1 h. The cooled reaction mixture was diluted with dichloromethane and methanol, filtered through a plug of Celite and the solvents were evaporated. The residue was purified by HPLC to give 36 mg (37 % Yield) of the title product.
情報源と証拠
| 出典データセット | 750 AstraZeneca ELN dataset |
|---|
| ORD ID | ord-e759108cf109420c9b96a1936ea5e56d |
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| 出典メモ | 750 AstraZeneca ELN dataset |
|---|