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1-Ethoxycarbonyl-4-(4-fluoro-2-nitroanilino)piperidine → 4-(2-Amino-4-fluoro-phenylamino)-piperidine-1-carboxylic acid ethyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-Ethoxycarbonyl-4-(4-fluoro-2-nitroanilino)piperidine | HCID 13792162 | — |
| 触媒 | Platinum | HCID 23939 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 4-(2-Amino-4-fluoro-phenylamino)-piperidine-1-carboxylic acid ethyl ester | HCID 13792172 | — |
反応手順
This 1-ethoxycarbonyl-4-(4-fluoro-2-nitroanilino)piperidine (5.7 g, 18.3 mmol.) was dissolved in THF (50 mL) and diluted with ethanol (100 mL). After addition of 5% platinum/carbon catalyst (1.2 g), the hydrogenation of the nitro functional group was carried out at atmospheric pressure via a balloon over a four hour period. The catalyst was removed and the solvents evaporated to give 1-ethoxycarbonyl-4-(2-amino-4-fluoroanilino)-piperidine as a viscous oil which was used as is.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05952351 |
| 出典データセット | uspto-grants-1999_09 |
| ORD ID | ord-b8a4a0d7860c41439dc09b23fbabf156 |
| 出典メモ | uspto-grants-1999_09 |