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HRID 59082作成日：2026年10月23日
Cesium carbonate → 4-(((3,3-Difluorocyclobutyl)methoxy)methyl)-6-(1-ethoxyvinyl)-N-(3-methoxy-4-(6-methylpyridazin-4-yl)phenyl)pyrimidin-2-amine
https://huagongshe.com/ja/reaction/59082
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 2-(Dicyclohexylphosphino)biphenyl | HCID 2734216 | — |
| 反応物 | 3-Methoxy-4-(6-methylpyridazin-4-yl)aniline | HCID 66859066 | — |
| 反応物 | 2-Chloro-4-(((3,3-difluorocyclobutyl)methoxy)methyl)-6-(1-ethoxyvinyl)pyrimidine | HCID 117820700 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 4-(((3,3-Difluorocyclobutyl)methoxy)methyl)-6-(1-ethoxyvinyl)-N-(3-methoxy-4-(6-methylpyridazin-4-yl)phenyl)pyrimidin-2-amine | HCID 117821096 | 104.3% |
反応手順
A mixture of 2-chloro-4-(((3,3-difluorocyclobutyl)methoxy)methyl)-6-(1-ethoxyvinyl)pyrimidine (0.068 g, 0.21 mmol), 3-methoxy-4-(6-methylpyridazin-4-yl)aniline (0.046 g, 0.21 mmol), cesium carbonate (0.139 g, 0.43 mmol), palladium (II) acetate (7 mg, 0.03 mmol) and (2-biphenylyl)dicyclohexylphosphine (0.011 g, 0.03 mmol) in dioxane (2 mL) was heated under argon at 120° C. for 90 min in microwave reactor. The mixture was filtered through a short silica plug and was eluted with 10% MeOH in EtOAc. The solvents were evaporated to give the title compound (0.109 g, quant).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US09439904B2 |
|---|
| 出典データセット | uspto-grants-2016_09 |
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| ORD ID | ord-2bc56a693ef549deb08355a270cdc4fc |
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| 出典メモ | uspto-grants-2016_09 |
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