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HRID 750686作成日:2026年10月25日

Benzyl Bromide → [3-(2-Benzyl-1,1-dioxo-1,2-dihydro-1lambda6-benzo[e][1,2,3]thiadiazin-4-yl)-5-fluoro-2-methyl-indol-1-yl]-acetic acid tert-butyl ester

https://huagongshe.com/reaction/750686

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tert-Butyl bromoacetateHCID 79177—
反応物4-(5-Fluoro-2-methyl-1H-indol-3-yl)-2H-benzo[e][1,2,3]thiadiazine 1,1-dioxideHCID 136388612—
溶媒WaterHCID 962—
溶媒AcetonitrileHCID 6342—
溶媒DichloromethaneHCID 6344—
生成物[3-(2-Benzyl-1,1-dioxo-1,2-dihydro-1lambda6-benzo[e][1,2,3]thiadiazin-4-yl)-5-fluoro-2-methyl-indol-1-yl]-acetic acid tert-butyl esterHCID 67315485—

反応条件

温度80 °C

反応手順

Benzyl bromide (10 μL, 67 μmol) and K2CO3 (10 mg, 72 μmol) were added to a solution of 4-(5-fluoro-2-methyl-1H-indol-3-yl)-2H-benzo[e][1,2,3]thiadiazine 1,1-dioxide (20 mg, 61 μmol) in CH3CN (1 mL), and stirred overnight at 80° C. An additional amount of K2CO3 (10 mg, 72 μmol) and tert-butyl bromoacetate (14 μL, 92 μmol) was added, and the reaction mixture stirred an additional 2 h at 80° C. The reaction mixture was diluted with H2O and CH2Cl2, and filtered through an Extrelut column. The Extrelut column was washed with CH2Cl2, and the filtrate was concentrated to afford the sub-title compound, which was carried onto the next step without further purification or characterization.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07405215B2
出典データセットuspto-grants-2008_07
ORD IDord-b812b79223404b1e9c0ad29aa19322ae
出典メモuspto-grants-2008_07