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Diisopropylethylamine → ethyl (2S)-2-(2-{4-[(2S)-2-hydroxy-3-(2-methylbenzothiazol-5-yloxy)propyl]piperazinyl}acetylamino)-2-(4-fluorophenyl)acetate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | (2S)-1-(2-methylbenzothiazol-5-yloxy)-3-piperazinylpropan-2-ol | HCID 58595334 | — |
| 反応物 | Ethyl (2S)-2-(2-chloroacetylamino)-2-(4-fluorophenyl)acetate | HCID 58719661 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | ethyl (2S)-2-(2-{4-[(2S)-2-hydroxy-3-(2-methylbenzothiazol-5-yloxy)propyl]piperazinyl}acetylamino)-2-(4-fluorophenyl)acetate | HCID 58719662 | — |
反応手順
Ethyl (2S)-2-(2-chloroacetylamino)-2-(4-fluorophenyl)acetate (400 mg, 1.46 mmol), (2S)-3-(2-methylbenzothiazol-5-yloxy)-1-piperazinylpropan-2-ol (560 mg, 1.46 mmol), and 1.26 ml diisopropylethylamine (7.3 mmol) was refluxed in ethanol for 24 hours. Solvent was removed under reduced pressure, and the residue purified by Prep TLC, to provide ethyl (2S)-2-(2-{4-[(2S)-2-hydroxy-3-(2-methylbenzothiazol -5-yloxy)propyl]piperazinyl}acetylamino)-2-(4-fluorophenyl)acetate.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07125876B2 |
| 出典データセット | uspto-grants-2006_10 |
| ORD ID | ord-ab6fdded6f034af3954218d3f94ff2c6 |
| 出典メモ | uspto-grants-2006_10 |