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2,4-Dichlorobenzylamine → 3-Quinolinecarboxamide,8-chloro-1-cyclopropyl-n-[(2,4-dichlorophenyl)methyl]-6,7-difluoro-1,4-dihydro-4-oxo-
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2,4-Dichlorobenzylamine | HCID 1485 | — |
| 反応物 | PyBOP | HCID 2724699 | — |
| 反応物 | 8-Chloro-1-cyclopropyl-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | HCID 9835941 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 3-Quinolinecarboxamide,8-chloro-1-cyclopropyl-n-[(2,4-dichlorophenyl)methyl]-6,7-difluoro-1,4-dihydro-4-oxo- | HCID 57780978 | — |
反応手順
15.0 g of 8-chloro-1-cyclopropyl-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (for preparation see DE 3420743 or Y. Kimura et al., J. Med. Chem. (1994) 37:3344) are dissolved in 500 ml of DMF and 31.3 g of PyBOP and 10.6 g of 2,4-dichlorobenzylamine are added. After a day the solvent is removed and the residue is purified by flash chromatography on silica gel (toluene/ethyl acetate 95:5).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07867992B2 |
| 出典データセット | uspto-grants-2011_01 |
| ORD ID | ord-2c3541e8cc8b4e2384b9f35fcb325080 |
| 出典メモ | uspto-grants-2011_01 |