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(2R,5R)-5-[(1S,2S)-1-benzyloxy-2-dibenzylamino-3-(3,5-difluorophenyl)-propyl]-2-(2,2-dimethylpropoxy)-morpholine-4-carboxylic acid tert-butyl ester → (2R,5R)-5-[(1S,2S)-2-Amino-3-(3,5-difluorophenyl)-1-hydroxypropyl]-2-(2,2-dimethylpropoxy)-morpholine-4-carboxylic acid tert-butyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | (2R,5R)-5-[(1S,2S)-1-benzyloxy-2-dibenzylamino-3-(3,5-difluorophenyl)-propyl]-2-(2,2-dimethylpropoxy)-morpholine-4-carboxylic acid tert-butyl ester | HCID 68559691 | — |
| 反応物 | HCID 178418361 | HCID 178418361 | — |
| 触媒 | Palladium hydroxide | HCID 9942167 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | (2R,5R)-5-[(1S,2S)-2-Amino-3-(3,5-difluorophenyl)-1-hydroxypropyl]-2-(2,2-dimethylpropoxy)-morpholine-4-carboxylic acid tert-butyl ester | HCID 68560376 | 93.5% |
反応手順
Stir (2R,5R)-5-[(1S,2S)-1-benzyloxy-2-dibenzylamino-3-(3,5-difluorophenyl)-propyl]-2-(2,2-dimethylpropoxy)-morpholine-4-carboxylic acid tert-butyl ester (0.1 g, 0.14 mmol) and 20% palladium hydroxide on carbon (0.1 g, 0.06 mmol, 60% moisture) in ethyl acetate (5 mL) under 1 atmosphere of hydrogen gas at room temperature overnight. Filter the suspension through a pad of filtering agent, wash with ethyl acetate and concentrate to give the title compound (0.06 g, 90%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07745438B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-cc8d9691ad97484190da0af67f9a81e6 |
| 出典メモ | uspto-grants-2010_06 |