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Tetrahydrofuran → N-{5-[(2-{[(2,2-difluorocyclopropyl)carbonyl]amino]imidazo[1,2-b]pyridazin-6-yl)oxy]-2-methylphenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Tetrahydrofuran | HCID 8028 | — |
| 反応物 | Oxalyl chloride | HCID 65578 | — |
| 反応物 | 2,2-Difluorocyclopropane-1-carboxylic acid | HCID 2782823 | — |
| 反応物 | N-{5-[(2-aminoimidazo[1,2-b]pyridazin-6-yl)oxy]-2-methylphenyl)-1,3-dimethyl-1H-pyrazole-5-carboxamide hydrochloride | HCID 57505635 | — |
| 触媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Dimethylacetamide | HCID 31374 | — |
| 生成物 | N-{5-[(2-{[(2,2-difluorocyclopropyl)carbonyl]amino]imidazo[1,2-b]pyridazin-6-yl)oxy]-2-methylphenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide | HCID 57505634 | 73% |
反応手順
In the same manner as in Example 259 and using 2,2-difluorocyclopropanecarboxylic acid (88 mg, 0.60 mmol), tetrahydrofuran (5 mL), N,N-dimethylformamide (1 drop), oxalyl chloride (74 μL, 0.86 mmol), N-{5-[(2-aminoimidazo[1,2-b]pyridazin-6-yl)oxy]-2-methylphenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide hydrochloride (250 mg, 0.60 mmol) and N,N-dimethylacetamide (7 mL) as starting materials, the title compound (210 mg, 73%) was obtained as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08034812B2 |
| 出典データセット | uspto-grants-2011_10 |
| ORD ID | ord-09c4a71f71e14641bf28ad0437712d97 |
| 出典メモ | uspto-grants-2011_10 |