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HRID 1162748作成日:2026年10月25日

1,1'-Carbonyldiimidazole → 2-(2-(3-(Trifluoromethyl)-4,5,6,7-tetrahydroindazole-1-yl)acetamido)thiophene-3-carboxamide

https://huagongshe.com/reaction/1162748

反応式

関与物質

役割名称HCID仕込み量
反応物1,1'-CarbonyldiimidazoleHCID 68263—
反応物2-Aminothiophene-3-carboxamideHCID 699495—
反応物[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetic acidHCID 788039—
溶媒dichloromethane N,N-dimethylformamideHCID 22350042—
生成物2-(2-(3-(Trifluoromethyl)-4,5,6,7-tetrahydroindazole-1-yl)acetamido)thiophene-3-carboxamideHCID 529415022%

反応条件

温度120 °C

反応手順

2-aminothiophene-3-carboxamide (23 mg, 0.16 mmol) and 2-(3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazole-1-yl)acetic acid (40 mg, 0.16 mmol) were dissolved in DCM/DMF (2 mL/50 μL) and polymer supported carbonyldiimidazole (264 mg, 1.2 mmol/g, 0.32 mmol) added. The reaction mixture was heated at 120° C. for 10 min in a Biotage SmithCreator microwave. The reaction mixture was filtered washing with MeOH (10 mL), EtOAc (10 mL), and MeCN (10 mL). The filtrate was concentrated in vacuo to give a yellow gum. Purification by preparative reverse phase HPLC gave desired product (1 mg, 2%).

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-31b1677b6eee4b349fa72a597452b90c
出典メモuspto-grants-2010_10