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3-Pyridinemethanamine → 4-[4-(Methylsulfonyl)phenyl]-N-(pyridin-3-ylmethyl)-6-(trifluoromethyl)pyrimidin-2-amine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3-Pyridinemethanamine | HCID 31018 | — |
| 反応物 | 2-(Methylsulfonyl)-4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)pyrimidine | HCID 11176443 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 4-[4-(Methylsulfonyl)phenyl]-N-(pyridin-3-ylmethyl)-6-(trifluoromethyl)pyrimidin-2-amine | HCID 10272842 | 94.2% |
反応手順
To a stirred solution of 2-(methylsulfonyl)-4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)pyrimidine (0.10 g, 0.26 mmol) in MeCN (3 ml) was added 3-(aminomethyl)-pyridine (169 mg, 6 eq) and the resultant solution heated under reflux for 3 h. The cooled reaction mixture was concentrated in vacuo and the resulting oil purified by SPE chromatography with chloroform then chloroform:methanol (50:1) as eluant. This gave the title compound as a yellow solid (100 mg, 93%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06780870B2 |
| 出典データセット | uspto-grants-2004_08 |
| ORD ID | ord-298d22e6944543f7b6e4fa2f33ce8528 |
| 出典メモ | uspto-grants-2004_08 |