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Sodium Carbonate → 5-(2,4-Dimethyl-oxazol-5-yl)-2,4-dimethoxy-pyrimidine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sodium Carbonate | HCID 10340 | — |
| 反応物 | Triphenylphosphine | HCID 11776 | — |
| 反応物 | (2,4-Dimethoxypyrimidin-5-yl)boronic acid | HCID 2736209 | — |
| 反応物 | 5-Iodo-2,4-dimethyl-oxazole | HCID 59337589 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 溶媒 | 1-Propanol | HCID 1031 | — |
| 生成物 | 5-(2,4-Dimethyl-oxazol-5-yl)-2,4-dimethoxy-pyrimidine | HCID 58994208 | 67.1% |
反応手順
2,4-Dimethoxy-pyrimidine-5-boronic acid (840 mg, 4.6 mmol) was dissolved in degassed n-PrOH (40 mL) and then 5-iodo-2,4-dimethyl-oxazole (Prep60, 850 mg, 3.8 mmol), Na2CO3 (848 mg, 8 mmol), PPh3 (332 mg, 1.3 mmol) and Pd(OAc)2 (85 mg, 0.38 mmol) were added. The suspension was stirred at reflux for 4 hours. The solvent was evaporated under vacuum and the crude was partitioned between water and ethyl acetate. The organic phase was dried (Na2SO4) and evaporated. The crude was purified by SCX cartridge to give 600 mg of the title compound (66% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07727988B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-49aa7eb002944783b9f978f9c7b080b9 |
| 出典メモ | uspto-grants-2010_06 |