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HRID 42137作成日:2026年10月26日

2-Amino-5-bromopyridine → N-(5-Bromopyridin-2-yl)-4-methanesulfonylbenzamide

https://huagongshe.com/reaction/42137

反応式

関与物質

役割名称HCID仕込み量
反応物2-Amino-5-bromopyridineHCID 70622—
反応物p-(Methylsulphonyl)benzoic acidHCID 77670—
反応物1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 2723939—
触媒4-(Dimethylamino)pyridineHCID 14284—
溶媒WaterHCID 962—
溶媒DichloromethaneHCID 6344—
生成物N-(5-Bromopyridin-2-yl)-4-methanesulfonylbenzamideHCID 6065097132%

反応手順

To a solution of 4-methanesulfonylbenzoic acid (100 mg, 0.50 mmol) and 2-amino-5-bromopyridine (104 mg, 0.60 mmol) in dry dichloromethane (10 mL) was added 4-(dimethylamino)pyridine (67 mg, 0.55 mmol) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (105 mg, 0.55 mmol). The mixture was stirred at room temperature overnight under N2, diluted with water (10 mL) and extracted with ethyl acetate. The organic layer was washed with brine, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform/ethyl acetate=3/1) to give the title compound as a white crystal (56 mg, yield 32%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08536176B2
出典データセットuspto-grants-2013_09
ORD IDord-4c00404d38ee45448ee89b81e24fc793
出典メモuspto-grants-2013_09