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1,8-Diazabicyclo(5.4.0)undec-7-ene → 1-Ethyl-6,8-difluoro-7-[2-(formylaminomethyl)morpholino]-1,4-dihydro-4-oxoquinoline-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-Ethyl-6,7,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | HCID 9835179 | — |
| 反応物 | 2-(Formylaminomethyl)morpholine hydrochloride | HCID 19834980 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 1-Ethyl-6,8-difluoro-7-[2-(formylaminomethyl)morpholino]-1,4-dihydro-4-oxoquinoline-3-carboxylic acid | HCID 14652602 | — |
反応手順
A solution of 813 mg of 1-ethyl-6,7,8-trifluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid, 650 mg of 2-(formylaminomethyl)morpholine hydrochloride and 1.0 g of 1,8-diazabicyclo[5.4.0]undec-7-ene in 10 ml of acetonitrile is refluxed for 3 hours and allowed to stand at room temperature overnight. The precipitated crystals are collected by filtration and successively washed with acetonitrile, water and acetone to give 1-ethyl-6,8-difluoro-7-[2-(formylaminomethyl)morpholino]-1,4-dihydro-4-oxoquinoline-3-carboxylic acid, melting at 234°-236° C.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US04889857 |
| 出典データセット | uspto-grants-1989_12 |
| ORD ID | ord-86916008a3a74584aa92e85bdd727e74 |
| 出典メモ | uspto-grants-1989_12 |