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2-(Trifluoromethyl)cinnamic acid, (E)- → N-[(S)-1-benzyl-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-N-(4-pentyl-benzyl)-3-(2-trifluoromethyl-phenyl)-acrylamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-(Trifluoromethyl)cinnamic acid, (E)- | HCID 719625 | — |
| 反応物 | 1-(4-benzyl-piperazin-1-yl)-(S)-2-(4-pentyl-benzylamino)-3-phenyl-propan-1-one | HCID 59808255 | — |
| 生成物 | N-[(S)-1-benzyl-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-N-(4-pentyl-benzyl)-3-(2-trifluoromethyl-phenyl)-acrylamide | HCID 67005290 | 61.3% |
反応手順
Acylation of 1-(4-benzyl-piperazin-1-yl)-(S)-2-(4-pentyl-benzylamino)-3-phenyl-propan-1-one (43.5 mg, 0.09 mmol) according to the procedure described for the preparation of Example 1 with trans-2-trifluoromethyl-cinnamic acid (21.4 mg, 0.099 mmol) gave 37.6 mg (60%) of N—[(S)-1-benzyl-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-N-(4-pentyl-benzyl)-3-(2-trifluoromethyl-phenyl)-acrylamide. LC-MS: tR=1.04 min; [M+H]+=682.49.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08067419B2 |
| 出典データセット | uspto-grants-2011_11 |
| ORD ID | ord-7e9e66307a6c413a9c7559b18d1798f9 |
| 出典メモ | uspto-grants-2011_11 |