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Sodium Carbonate → 4-Chloro-6-(5-chloro-2-methoxy-phenyl)-pyrimidin-2-yl-amine
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-Amino-4,6-dichloropyrimidine | HCID 65522 | — |
| 反応物 | 5-Chloro-2-methoxyphenylboronic acid | HCID 2735751 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | 1,2-Dimethoxyethane | HCID 8071 | — |
| 生成物 | 4-Chloro-6-(5-chloro-2-methoxy-phenyl)-pyrimidin-2-yl-amine | HCID 86004313 | 58.1% |
反応手順
To a mixture of 4,6-dichloro-pyrimidin-2-yl-amine (0.304 g, 2.0 mmol), 5-chloro-2-methoxy-phenyl boronic acid (0.373 g, 2.0 mmol), palladium (II) acetate (0.068 g, 0.30 mmol) and triphenylphosphine (0.157 g, 0.60 mmol) was added a solution of sodium carbonate (1.36 g, 12.8 mmol) in water (5 ml) followed by glyme (20 ml). The mixture was stirred under an atmosphere of argon for 1 hour. Filtration and concentration of the filtrate provided a residue which was purified by flash chromatography on silica gel eluting with ethyl acetate-hexane (1:3) to provide 4-chloro-6-(5-chloro-2-methoxy-phenyl)-pyrimidin-2-yl-amine (0.314 g, 58% yield) as a white powder.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07419984B2 |
| 出典データセット | uspto-grants-2008_09 |
| ORD ID | ord-3e25d25f62b4403faefdd8ecc811df39 |
| 出典メモ | uspto-grants-2008_09 |