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HRID 1943472作成日：2026年10月27日
3-Amino-5-methylisoxazole → 6-chloro-N-(3-fluoropyridin-4-yl)-8-(5-methylisoxazol-3-ylamino)imidazo[1,2-b]pyridazine-3-carboxamide
https://huagongshe.com/reaction/1943472
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 3-Amino-5-methylisoxazole | HCID 66172 | — |
| 反応物 | Sodium t-butoxide | HCID 23676156 | — |
| 反応物 | 8-Bromo-6-chloro-N-(3-fluoropyridin-4-yl)imidazo[1,2-b]pyridazine-3-carboxamide | HCID 59624495 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 6-chloro-N-(3-fluoropyridin-4-yl)-8-(5-methylisoxazol-3-ylamino)imidazo[1,2-b]pyridazine-3-carboxamide | HCID 86649271 | 48.2% |
反応手順
A mixture of 5A (40 mg, 0.123 mmol), 5-methylisoxazol-3-amine (30.1 mg, 0.307 mmol) and sodium t-butoxide (29.5 mg, 0.307 mmol) in THF (1.5 mL) was heated at 70° C. for 2 h, the cooled to room temperature. The solvent was removed and the residue was purified by ISCO column chromatography (4 g column, MeOH/DCM=0-10%) to give 51A (23 mg, 48%). HPLC Rt=3.043 min (Chromolith SpeedROD 4.6×50 mm, 10-90% aqueous methanol containing 0.1% TFA, 4 min gradient, monitored at 220 nm), [M+H]=388.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08389527B2 |
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| 出典データセット | uspto-grants-2013_03 |
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| ORD ID | ord-065ce67624804506b21135dc68200e45 |
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| 出典メモ | uspto-grants-2013_03 |
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