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Butanoic acid, 4-chloro-4-oxo-, methyl ester → 4-[3-(3-Fluoro-phenylamino)-6,7-dimethoxy-4H-indeno[1,2-c]pyrazol-1-yl]-4-oxo-butyric acid methyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Butanoic acid, 4-chloro-4-oxo-, methyl ester | HCID 73888 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | Jnj-10198409 | HCID 9797370 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 4-[3-(3-Fluoro-phenylamino)-6,7-dimethoxy-4H-indeno[1,2-c]pyrazol-1-yl]-4-oxo-butyric acid methyl ester | HCID 58824826 | — |
反応手順
To a mixture of (6,7-Dimethoxy-1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-(3-fluoro-phenyl)-amine (Compound 14) (0.50 g, 1.5 mmol), 3-Chlorocarbonyl-propionic acid methyl ester (Compound 26a) (0.277 g, 1.8 mmole) and DMF (1.5 mL) was added Diisopropylethylamine (DIEA) (0.52 mL, 3.0 mmole) at room temperature with stirring. The reaction was stirred at room temperature over night. The reaction was quenched with water and extracted with EtOAc. The solvent was removed via rotovap and the crude material was prepped on the reverse phase HPLC. Lyophilization gave the title compound as a white powder. MS m/z439.9 (M+H)+;
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07196110B2 |
| 出典データセット | uspto-grants-2007_03 |
| ORD ID | ord-3032bbf713c84279888a4b6191ba6e7f |
| 出典メモ | uspto-grants-2007_03 |