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2-(4-Fluorophenyl)piperazine → (RS)-3-ethoxycarbonyl-7,9-difluoro-8-[3-(4-fluorophenyl)-1-piperazinyl]-1-methyl-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-(4-Fluorophenyl)piperazine | HCID 4617623 | — |
| 反応物 | 3-Ethoxycarbonyl-7,8,9-trifluoro-1-methyl-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine | HCID 19423688 | — |
| 生成物 | 1,8-Naphthyridine | HCID 136069 | — |
| 生成物 | (RS)-3-ethoxycarbonyl-7,9-difluoro-8-[3-(4-fluorophenyl)-1-piperazinyl]-1-methyl-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine | HCID 53817874 | 142.2% |
反応手順
(RS)-3-Ethoxycarbonyl-7,9-difluoro-8-[3-(4-fluorophenyl)-1-piperazinyl]-1-methyl-4-oxo -1,4-dihydrobenzo[9 [1,8]naphthyridine was prepared under the conditions of Example 39, but starting with 3-ethoxycarbonyl-7,8,9-trifluoro-1-methyl-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine (2 g) and (RS)-2-(4-fluorophenyl)piperazine (4 g). After 1 recrystallization in a mixture of dimethylformamide (3.5 cc) and ethanol (31.5 cc), (RS)-3-ethoxycarbonyl-7,9-difluoro-8-[3-(4-fluorophenyl)-1-piperazinyl]-1-methyl-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine (2.1 g) is obtained in the form of a beige solid, m.p. 242° C.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05053509 |
| 出典データセット | uspto-grants-1991_10 |
| ORD ID | ord-b9f6612d87784214ae500d1b4b1027db |
| 出典メモ | uspto-grants-1991_10 |