関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 4-Chloroaniline | HCID 7812 | — |
| 反応物 | Binap, (A+-)- | HCID 634876 | — |
| 反応物 | Sodium t-butoxide | HCID 23676156 | — |
| 反応物 | 4-Chloro-6-(5-chloro-2-methoxyphenyl)-2-methylpyrimidine | HCID 65645326 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | [6-(5-Chloro-2-methoxy-phenyl)-2-methyl-pyrimidin-4-yl]-(4-chloro-phenyl)-amine | HCID 42606283 | 51% |
反応手順
To an argon saturated solution of 4-chloro-6-(5-chloro-2-methoxy-phenyl)-2-methyl-pyrimidine (50 mg, 0.18 mmol), 4-chloroaniline (23 mg, 0.18 mmol), rac-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (66 mg, 0.1 mmol) and sodium tert-butoxide (26 mg, 0.27 mmol) in toluene (10 ml) was added tris(dibenzylideneacetone)-dipalladium (92 mg, 0.1 mmol). After stirring at 80° C. under an argon atmosphere for 6 hours, the mixture was concentrated under vacuum. The residue was purified by flash chromatography on silica gel eluting with ethyl acetate-hexane (1:5 followed by 1:3) to provide the title compound (33 mg, 51% yield) as a white powder.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07419984B2 |
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| 出典データセット | uspto-grants-2008_09 |
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| ORD ID | ord-7e375155c85249418ae34867e8f15bf8 |
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| 出典メモ | uspto-grants-2008_09 |
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