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(2,3-Dihydrobenzofuran-2-yl)methanamine → (6-Chloro-2-methoxy-pyrimidin-4-yl)-(2,3-dihydro-benzofuran-2-ylmethyl)-amine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | (2,3-Dihydrobenzofuran-2-yl)methanamine | HCID 29905 | — |
| 反応物 | Sodium Bicarbonate | HCID 516892 | — |
| 反応物 | 4,6-Dichloro-2-methoxypyrimidine | HCID 12052160 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | (6-Chloro-2-methoxy-pyrimidin-4-yl)-(2,3-dihydro-benzofuran-2-ylmethyl)-amine | HCID 86615711 | 74.5% |
反応手順
A mixture of 4,6-dichloro-2-methoxy-pyrimidine (0.41 g, 2.3 mmol), C-(2,3-dihydro-benzofuran-2-yl)-methylamine (0.52 g, 3.47 mmol), and NaHCO3 (0.97 g, 12 mmol) in EtOH (7 mL) is heated to reflux for 3 h. The mixture is diluted with water (8 mL), filtered, washed (water). The solid is dissolved in EtOAc, dried (MgSO4), filtered, and concentrated in vacuo to afford (6-chloro-2-methoxy-pyrimidin-4-yl)-(2,3-dihydro-benzofuran-2-ylmethyl)-amine (0.5 g) as a solid. LCMS: RT=2.59 minutes; MS: 292 (M+H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08193183B2 |
| 出典データセット | uspto-grants-2012_06 |
| ORD ID | ord-3f637824f985437ca2038a7215147eab |
| 出典メモ | uspto-grants-2012_06 |