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1,8-Diazabicyclo(5.4.0)undec-7-ene → 7-(3-Aminomethyl-4-methyl-1-pyrrolidinyl)-6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1,8-Diazabicyclo(5.4.0)undec-7-ene | HCID 81184 | — |
| 反応物 | (4-Methylpyrrolidin-3-yl)methanamine | HCID 4583498 | — |
| 反応物 | 1-(2-Fluoroethyl)-6,7,8-trifluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid | HCID 12770908 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 7-(3-Aminomethyl-4-methyl-1-pyrrolidinyl)-6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid | HCID 13933091 | 67.9% |
反応手順
A mixture of 6,7,8-trifluoro-1-(2-fluoroethyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (0.5 g), anhydrous acetonitrile (5 ml), 3-aminomethyl-4-methylpyrrolidine (0.21 g) and DBU (0.26 g) was refluxed for an hour and then stirred at room temperature for 5 hours. The resulting precipitate was collected by filtration and washed with ether to give the title compound (0.45 g) as pale yellow powder, mp 228°-232° C.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US04753953 |
| 出典データセット | uspto-grants-1988_06 |
| ORD ID | ord-1274400261fc4b1b91dac3ea22c0802c |
| 出典メモ | uspto-grants-1988_06 |