化工社化工社 化学情報印刷レポート · 研究参考用
1,8-Diazabicyclo(5.4.0)undec-7-ene → 1-Cyclopropyl-6-fluoro-8-methoxy-7-{3-[(methylamino)methyl]pyrrolidin-1-yl}-4-oxo-1,4-dihydroquinoline-3-carboxylic 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 | 1-Cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid | HCID 7019465 | — |
| 反応物 | N-Methyl-1-(pyrrolidin-3-yl)methanamine | HCID 13491795 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 1-Cyclopropyl-6-fluoro-8-methoxy-7-{3-[(methylamino)methyl]pyrrolidin-1-yl}-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | HCID 483413 | 49.3% |
反応手順
A mixture of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid (200 mg), 3-methylaminomethylpyrrolidine (90 mg), DBU (110 mg) and anhydrous acetonitrile (3 ml) was refluxed for 75 minutes. After cooling, the resulting precipitate was collected by filtration and recrystallized from a solution of dichloromethane-methanol (1:1) to give the title compound (130 mg) as white powdery crystals, mp 226.5°-230° C.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05043450 |
| 出典データセット | uspto-grants-1991_08 |
| ORD ID | ord-df923ee056214776bad916cd779a74a0 |
| 出典メモ | uspto-grants-1991_08 |