関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Triphosgene | HCID 94429 | — |
| 反応物 | 1-(1,3-Thiazol-2-yl)ethan-1-amine | HCID 19896985 | — |
| 反応物 | 4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyaniline | HCID 21891031 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Chloroform | HCID 6212 | — |
| 生成物 | Ki-20227 | HCID 9869779 | 144.3% |
反応手順
4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2-methoxyaniline (816 mg) was dissolved in chloroform (40 ml) and triethylamine (2.0 ml) to prepare a solution. A solution of triphosgene (368 mg) in chloroform (1.0 ml) was then added to the solution, and the mixture was stirred at room temperature for one hr. Next, a solution of 1-(1,3-thiazol-2-yl)-1-ethylamine (352 mg) in chloroform (1.0 ml) was added thereto, and the mixture was stirred at room temperature overnight. Water (40 ml) was added thereto, and the mixture was stirred for 10 min, followed by extraction with chloroform. The organic layer was washed with saturated brine and was dried over sodium sulfate. The solvent was removed by evaporation, and the residue was purified by chromatography on silica gel using chloroform/acetone for development to give the title compound (860 mg, 72%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07598258B2 |
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| 出典データセット | uspto-grants-2009_10 |
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| ORD ID | ord-bf53e52bd87842938aea537518b4ce1b |
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| 出典メモ | uspto-grants-2009_10 |
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