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HRID 425430作成日:2026年10月25日

Stannane → 4-(2,2-dimethylpropyl)-2-{1-[4-(5-fluoropyridin-2-yl)benzyl]vinyl}-N,N-dimethyl-1H-imidazole-1-sulfonamide

https://huagongshe.com/reaction/425430

反応式

関与物質

役割名称HCID仕込み量
反応物StannaneHCID 123161—
反応物2-Bromo-5-fluoropyridineHCID 2783171—
反応物2-[1-(4-bromobenzyl)vinyl]-4-(2,2-dimethylpropyl)-N,N-dimethyl-1H-imidazole-1-sulfonamideHCID 66705618—
触媒HCID 178418397HCID 178418397—
溶媒1,2-DimethoxyethaneHCID 8071—
溶媒Ethyl AcetateHCID 8857—
生成物4-(2,2-dimethylpropyl)-2-{1-[4-(5-fluoropyridin-2-yl)benzyl]vinyl}-N,N-dimethyl-1H-imidazole-1-sulfonamideHCID 66705844—

反応条件

温度90 °C

反応手順

Pd(PPh3)4 (196 mg) was added to a solution of 2-bromo-5-fluoropyridine in DME (10 mL) at ambient temperature. After heating at 90° C. overnight the reaction mixture was cooled. 2-[1-(4-bromobenzyl)vinyl]-4-(2,2-dimethylpropyl)-N,N-dimethyl-1H-imidazole-1-sulfonamide (110 mg) was added to the stannane solution followed by Pd(PPh3)4 (100 mg). After stirring at 95° C. overnight, the reaction mixture was cooled, diluted with ethyl acetate and washed with water. The organic phase was dried (sodium sulfate) and concentrated. Chromatography of the resulting crude product over silica eluting with 0-50% ethyl acetate/hexanes afforded 4-(2,2-dimethylpropyl)-2-{1-[4-(5-fluoropyridin-2-yl)benzyl]vinyl}-N,N-dimethyl-1H-imidazole-1-sulfonamide.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08106070B2
出典データセットuspto-grants-2012_01
ORD IDord-6057f7179c1c4696909845307f399c60
出典メモuspto-grants-2012_01