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HRID 242作成日:2026年10月23日

3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline → 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

https://huagongshe.com/ja/reaction/242

反応式

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)anilineHCID 45480181—
反応物8-Chloro-4-methyl-2-phenyl-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepineHCID 59577866—
試薬Cesium carbonateHCID 10796—
触媒2-(Dicyclohexylphosphino)biphenylHCID 2734216—
触媒Palladium (II) acetateHCID 4144353—
溶媒1,2-DimethoxyethaneHCID 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-amineHCID 4981993537.23%

反応条件

温度100 °C

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 IDord-e759108cf109420c9b96a1936ea5e56d
出典メモ750 AstraZeneca ELN dataset