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1,8-Diazabicyclo(5.4.0)undec-7-ene → 7-(3-t-Butoxycarbonylamino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-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 | 1-Cyclopropyl-6,7,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | HCID 535414 | — |
| 反応物 | tert-Butyl (4-methylpyrrolidin-3-yl)carbamate | HCID 14738853 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 7-(3-t-Butoxycarbonylamino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid | HCID 13933101 | 39.1% |
反応手順
A mixture of 1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (0.5 g), anhydrous acetonitrile (5 ml), 3-t-butoxycarbonylamino-4-methylpyrrolidine (0.53 g) and DBU (0.27 g) was refluxed for an hour. After cooling in a refrigerator, the resulting precipitate was collected by filtration and washed with acetonitrile and ether successively to give the title compound (0.32 g) as pale yellow powder, mp 230°-231° 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-99e9189c0ddf4dc5bd7e91caf10a1432 |
| 出典メモ | uspto-grants-1988_06 |