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HRID 502作成日:2026年10月23日

Aniline → Methyl 3-anilino-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate

https://huagongshe.com/ja/reaction/502

反応式

関与物質

役割名称HCID仕込み量
反応物AnilineHCID 6115—
反応物Methyl 3-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoateHCID 56973098—
試薬Potassium Phosphate, TribasicHCID 62657—
触媒Tris(1,1-dimethylethyl)phosphineHCID 83681—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒1,2-DimethoxyethaneHCID 8071—
生成物Methyl 3-anilino-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoateHCID 116889320%

反応条件

温度100 °C

反応手順

aniline (0.360 mL, 3.95 mmol) was added to methyl 3-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate (900 mg, 3.03 mmol), TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM(0) (139 mg, 0.15 mmol), [Reactants] and potassium phosphate (1546 mg, 7.28 mmol) in degassed DME (10 mL) at 20°C under nitrogen. The reaction was stirred at 100 °C for 24 hours. The reaction mixture was allowed to cool then filtered through celite, washing with ethyl acetate. The filtrate was evaporated under reduced pressure to give a brown residue. Not progressed any further.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-7f4bd58c1e854ed5b839b01e20dd39d2
出典メモ750 AstraZeneca ELN dataset