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HRID 62817作成日:2026年10月24日

Benzyl Bromide → 3-[Benzyl-(pyridine-3-sulfonyl)-amino]-benzoic acid

https://huagongshe.com/ja/reaction/62817

反応式

関与物質

役割名称HCID仕込み量
反応物Benzyl BromideHCID 7498—
反応物Cesium carbonateHCID 10796—
反応物3-(Pyridine-3-sulfonylamino)-benzoic acid tert-butyl esterHCID 67310872—
溶媒DimethylformamideHCID 6228—
溶媒Ethyl AcetateHCID 8857—
溶媒Trifluoroacetic acid methylene chlorideHCID 21863450—
生成物3-[Benzyl-(pyridine-3-sulfonyl)-amino]-benzoic acidHCID 6731078953.1%

反応手順

A solution of 3-(Pyridine-3-sulfonylamino)-benzoic acid tert-butyl ester (99 mg, 0.3 mmol), benzyl bromide (39 μL, 0.32 mmol) and Cesium Carbonate (145 mg, 0.4 mmol) in dimethylformamide (5 ml) was stirred for 16 hrs. The reaction was diluted with ethyl acetate (50 ml) and washed with water (6×100 ml). The organic layer was separated, dried over magnesium sulfate and concentrated in vacuo to give a yellow oil. The oil was dissolved in trifluoroacetic acid/dichloromethane (1:5 v/v) (10 ml), stirred for 3 hrs and then concentrated in vacuo to afford the title compound as a white solid (58.7 mg). HPLC retention time 4.31 min. Mass spectrum (APCI+) m/z 369 (M+H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09447033B2
出典データセットuspto-grants-2016_09
ORD IDord-95c46d306a314f198fa1f310bd5902d8
出典メモuspto-grants-2016_09