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HRID 1162757作成日:2026年10月26日

Potassium Carbonate → 2-(2-(4-(2-Hydroxyethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide

https://huagongshe.com/reaction/1162757

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物2-(2-Bromoacetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamideHCID 59520523—
反応物HCID 178520360HCID 178520360—
溶媒MethanolHCID 887—
溶媒DimethylformamideHCID 6228—
生成物2-(2-(4-(2-Hydroxyethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamideHCID 5952047741%

反応条件

温度60 °C

反応手順

To a solution of 2-(3-trifluoromethylpyrazol-4-yl)-ethanol (18 mg, 0.1 mmol) in DMF (0.5 mL) was added potassium carbonate (16 mg, 0.12 mmol). The reaction mixture was stirred at 60° C. for 25 min before 2-(2-bromoacetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (32 mg, 0.1 mmol) was added. Heating at 60° C. was maintained for 4 h before the reaction mixture was allowed to cool to RT. The whole was diluted with MeOH (0.5 mL), and filtered before being purified by preparative reverse phase HPLC to give the desired product as a white solid (17 mg, 0.04 mmol, 41%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07820707B2
出典データセットuspto-grants-2010_10
ORD IDord-433775414135442888f91eb145454deb
出典メモuspto-grants-2010_10