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Cesium carbonate → (R)-7-(4-morpholinophenyl)-N-((4-(pyrimidin-2-yl)morpholin-2-yl)methyl)pyrido[4,3-b]pyrazin-5-amine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 2-Bromopyrimidine | HCID 78345 | — |
| 反応物 | (S)-N-(morpholin-2-ylmethyl)-7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-amine | HCID 71113404 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | (R)-7-(4-morpholinophenyl)-N-((4-(pyrimidin-2-yl)morpholin-2-yl)methyl)pyrido[4,3-b]pyrazin-5-amine | HCID 71113950 | — |
反応手順
A solution of (S)—N-(morpholin-2-ylmethyl)-7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-amine (100 mg, 0.246 mmol), 2-bromopyrimidine (59 mg, 0.37 mmol) and cesiumcarbonate (193 mg, 0.592 mmol) in DMF (2 mL) was heated at 100° C. in a sealed tube for overnight. Then the mixture was extracted with EA, washed with brine, concentrated and purified by flash column chromatography, eluting with DCM/MeOH to give product as light yellow solid. MS (m/z): 485 (M+H)+
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09434726B2 |
| 出典データセット | uspto-grants-2016_09 |
| ORD ID | ord-ef64dc99c85f443da08f1a0eda8e388a |
| 出典メモ | uspto-grants-2016_09 |