関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Hydrochloric Acid | HCID 313 | — |
| 反応物 | Isopropanol | HCID 3776 | — |
| 反応物 | 5-Amino-4-fluoro-2-methylphenol | HCID 10154098 | — |
| 反応物 | 4-Chloro-6-methoxy-7-[(1-methylimidazol-2-yl)methoxy]cinnoline | HCID 21991019 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | 2-Pentanol | HCID 22386 | — |
| 生成物 | 4-(2-Fluoro-5-hydroxy-4-methylanilino)-6-methoxy-7-[(1-methylimidazol-2-yl)methoxy]cinnoline hydrochloride | HCID 21991024 | 79.5% |
反応手順
A suspension of 4-chloro-6-methoxy-7-[( 1-methylimidazol-2-yl)methoxy]cinnoline (109 mg, 0.35 mmol) and 2-fluoro-5-hydroxy-4-methylaniline (70 mg, 0.5 mmol), (prepared as described for the starting material in Example 11), in 2-pentanol (3 ml), DMF (0.5 ml) and a 5M solution of hydrogen chloride in isopropanol (74 μl, 0.35 mmol) was heated at reflux for 3 hours. The solution was then cooled to 0° C. and the resulting solid filtered off and washed with ether to give 4-(2-fluoro-5-hydroxy-4-methylanilino)-6-methoxy-7-[(1-methylimidazol-2-yl)methoxy]cinnoline hydrochloride as a yellow solid (124 mg, 73%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US07087602B2 |
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| 出典データセット | uspto-grants-2006_08 |
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| ORD ID | ord-1ef1353ef9b0448aa2e55a73c9130f30 |
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| 出典メモ | uspto-grants-2006_08 |
|---|
