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HRID 691作成日:2026年10月23日

1-Bromo-4-(methylsulphonyl)benzene → tert-butyl (2R)-2-methyl-4-(4-methylsulfonylphenyl)piperazine-1-carboxylate

https://huagongshe.com/ja/reaction/691

反応式

関与物質

役割名称HCID仕込み量
反応物1-Bromo-4-(methylsulphonyl)benzeneHCID 77014—
反応物tert-Butyl (2R)-2-methylpiperazine-1-carboxylateHCID 10262201—
試薬Potassium tert-butoxideHCID 23665647—
触媒Tris(1,1-dimethylethyl)phosphineHCID 83681—
触媒Bis(tri-tert-butylphosphine)palladium(0)HCID 2734558—
溶媒1,4-DioxaneHCID 31275—
生成物tert-butyl (2R)-2-methyl-4-(4-methylsulfonylphenyl)piperazine-1-carboxylateHCID 1334995780%

反応条件

温度100 °C

反応手順

13-May-09 10:32:28 +0100 1-bromo-4-(methylsulfonyl)benzene (515 mg, 2.13 mmol), (R)-tert-butyl 2-methylpiperazine-1-carboxylate (426 mg, 2.13 mmol) and BIS(TRI-T- BUTYLPHOSPHINE)PALLADIUM(0) (54.3 mg, 0.11 mmol) and potassium 2-methylpropan-2-olate (352 mg, 2.98 mmol) were suspended in dioxane (10 mL) and heated to 90°C for 3 hours. LC-MS shows starting material. Reaction abandoned.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-8f20cf3b966d4cdd9e1178539b8e969e
出典メモ750 AstraZeneca ELN dataset