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Sodium hydride → A2A receptor antagonist 1
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sodium hydride | HCID 24758 | — |
| 反応物 | alpha-Bromo-o-fluorotoluene | HCID 67968 | — |
| 反応物 | 4-(2-Furyl)-1H-pyrazolo[3,4-d]pyrimidine-6-amine | HCID 22015500 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | A2A receptor antagonist 1 | HCID 9879687 | 80.8% |
反応手順
A solution of 4-(2-furyl)-1H-pyrazolo[3,4-d]pyrimidine-6-amine (219 mg, 1 mmol) in DMF (2 mL) at 0° C. was treated with NaH (40 mg, 60%, 1 mmol), stirred for 20 min, treated with 2-fluorobenzyl bromide (120 μL, 1 mmol), stirred at room temperature for 1 h, quenched with water, extracted with EtOAc, dried (MgSO4), concentrated in vacuo and purified by chromatography EtOAc:Heptane, 1:4) to give the title compound (250 mg, 76%) as a cream solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07087754B2 |
| 出典データセット | uspto-grants-2006_08 |
| ORD ID | ord-362e4095935e451682d284f45f1e4e43 |
| 出典メモ | uspto-grants-2006_08 |