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phenylalaninol, (S)- → N-[(1S)-1-Benzyl-2-hydroxyethyl]-(2S)-2-[3-fluoro-4-(methylsulfonylamino)phenyl]propionamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | phenylalaninol, (S)- | HCID 447213 | — |
| 反応物 | 2-[3-Fluoro-4-(metylsulfonylamino)phenyl]propion | HCID 131731183 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-[(1S)-1-Benzyl-2-hydroxyethyl]-(2S)-2-[3-fluoro-4-(methylsulfonylamino)phenyl]propionamide | HCID 24754390 | — |
反応手順
A mixture of 2-[3-fluoro-4-(methylsulfonylamino)phenyl]propion acid (100 mg, 0.234 mmol) and L-phenyl alaninol (71 mg, 0.468 mmol) in CH2Cl2 (3 mL) was refluxed for 3 h and concentrated in vacuo. The residue was dissolved in MeOH (2 mL) and purified by flash column chromatography on silica gel using EtOAc:hexanes (2:1) to EtOAc:MeOH (20:1) as eluant to afford N-[(1S)-1-Benzyl-2-hydroxyethyl]-(2S)-2-[3-fluoro-4-(methylsulfonylamino)phenyl]propionamide.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08642657B2 |
| 出典データセット | uspto-grants-2014_02 |
| ORD ID | ord-09c0895840e8457380f08d0de98eabe0 |
| 出典メモ | uspto-grants-2014_02 |