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HRID 512501作成日:2026年10月26日

Benzyl Bromide → 1-Benzyl-6-methyl-4-oxo-5-(3-trifluoromethyl-phenyl)-1,4-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamide

https://huagongshe.com/reaction/512501

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Potassium CarbonateHCID 11430—
反応物6-Methyl-4-oxo-5-(3-trifluoromethyl-phenyl)-1,4-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamideHCID 86711533—
溶媒MethanolHCID 887—
溶媒DimethylformamideHCID 6228—
生成物1-Benzyl-6-methyl-4-oxo-5-(3-trifluoromethyl-phenyl)-1,4-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamideHCID 73426729—

反応条件

温度80 °C

反応手順

A mixture of 6-methyl-4-oxo-5-(3-trifluoromethyl-phenyl)-1,4-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamide (preparation 5, 50 mg, 0.108 mmol), K2CO3 (27 mg, 0.193 mmol) and benzyl bromide (0.015 mL, 0.129 mmol) in DMF (0.5 mL) is stirred for 30 min at 80° C. (microwave). The reaction mixture is diluted with MeOH, filtered and purified by preparative reversed-phase HPLC (XBridge, gradient of methanol in water, 0.3% NH4OH, 60° C.). Yield: 28 mg (47% of theory); ESI mass spectrum: [M+H]+=555; Retention time HPLC: 1.16 min (Z003—001).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09102624B2
出典データセットuspto-grants-2015_08
ORD IDord-095cce7bb2574db1aede192edde3f04f
出典メモuspto-grants-2015_08