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HRID 716作成日:2026年10月23日

Benzene, 4-bromo-1,2-dimethoxy- → tert-butyl (2R)-4-(3,4-dimethoxyphenyl)-2-propan-2-ylpiperazine-1-carboxylate

https://huagongshe.com/ja/reaction/716

反応式

関与物質

役割名称HCID仕込み量
反応物Benzene, 4-bromo-1,2-dimethoxy-HCID 76114—
反応物(R)-1-Boc-2-isopropylpiperazineHCID 24820392—
試薬Sodium t-butoxideHCID 23676156—
触媒2-(Dicyclohexylphosphino)-2'-(dimethylamino)biphenylHCID 2734217—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒TolueneHCID 1140—
生成物tert-butyl (2R)-4-(3,4-dimethoxyphenyl)-2-propan-2-ylpiperazine-1-carboxylateHCID 6909881260%

反応条件

温度150 °C

反応手順

21-Apr-09 08:58:54 +0100 4-bromo-1,2-dimethoxybenzene (0.135 mL, 0.92 mmol), (R)-tert-butyl 2-isopropylpiperazine-1-carboxylate (252 mg, 1.11 mmol) and 2-Dicyclohexylphosphino-2'-(N,N-dimethylamino)biphenyl (10.88 mg, 0.03 mmol) and Sodium tert-butoxide (128 mg, 1.29 mmol) and Tris(dibenzylideneacetone)dipalladium(0) (21.09 mg, 0.02 mmol) were suspended in toluene (5 mL) and sealed into a microwave tube. The reaction was heated to 150 °C for 30 minutes in the microwave reactor and cooled to RT. LC-MS show sproduct at 60% and SM 33% reaction mixture to be combined with EN02263-45 and worked up.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-8ac590d4cc01454e9f3c19a34317cb92
出典メモ750 AstraZeneca ELN dataset