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Tetrahydrofuran → N-[5-(5-Cyanopyridin-3-ylethynyl)-2-fluorophenyl]-isobutyramide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Tetrahydrofuran | HCID 8028 | — |
| 反応物 | Ethyl Acetate | HCID 8857 | — |
| 反応物 | 5-(3-Amino-4-fluorophenylethynyl)-nicotinonitrile | HCID 67047822 | — |
| 生成物 | N-[5-(5-Cyanopyridin-3-ylethynyl)-2-fluorophenyl]-isobutyramide | HCID 67047872 | 84% |
反応手順
Add a solution of isobutynyl chloride (0.09 g, 1.08 mmol) dissolved in tetrahydrofuran to a solution of 5-(3-amino-4-fluorophenylethynyl) -nicotinonitrile, (prepared as described in EXAMPLE 160), (0.2 g, 0.8 mmol) in anhydrous tetrahydrofuran and stir overnight at room temperature. Pour into ethyl acetate, wash with water and an aqueous saturated solution of sodium chloride, dry (potassium carbonate), filter and concentrate. Purify the residue by silica gel chromatography, eluting with 100:0 to 95:5 dichloromethane:ethyl acetate, to give the title compound as a white solid (210 mg, 84%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07915424B2 |
| 出典データセット | uspto-grants-2011_03 |
| ORD ID | ord-2e81bec6aa2e4ab89ae75b6cede69755 |
| 出典メモ | uspto-grants-2011_03 |