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5-(R)-[1-(S)-benzyloxy-3-(3-benzyloxyphenyl)-2-(R)-dibenzylaminopropyl]-2-(R)-(2,2-dimethylpropoxy)-3-(S)-methylmorpholine-4-carboxylic acid tert-butyl ester → 5-(R)-[2-(S)-Amino-1-(S)-hydroxy-3-(3-hydroxyphenyl)-propyl]-2-(R)-(2,2-dimethylpropoxy)-3-(S)-methylmorpholine-4-carboxylic acid tert-butyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-(R)-[1-(S)-benzyloxy-3-(3-benzyloxyphenyl)-2-(R)-dibenzylaminopropyl]-2-(R)-(2,2-dimethylpropoxy)-3-(S)-methylmorpholine-4-carboxylic acid tert-butyl ester | HCID 68563692 | — |
| 反応物 | HCID 178418361 | HCID 178418361 | — |
| 触媒 | Palladium hydroxide | HCID 9942167 | — |
| 溶媒 | tert-Butanol | HCID 6386 | — |
| 生成物 | 5-(R)-[2-(S)-Amino-1-(S)-hydroxy-3-(3-hydroxyphenyl)-propyl]-2-(R)-(2,2-dimethylpropoxy)-3-(S)-methylmorpholine-4-carboxylic acid tert-butyl ester | HCID 68561574 | 104.2% |
反応手順
Dissolve 5-(R)-[1-(S)-benzyloxy-3-(3-benzyloxyphenyl)-2-(R)-dibenzylaminopropyl]-2-(R)-(2,2-dimethylpropoxy)-3-(S)-methylmorpholine-4-carboxylic acid tert-butyl ester (1.38 g, 1.70 mmol) in tert-butanol (˜50 mL). Add 20% palladium hydroxide on carbon (4 g) and hydrogenate at 50 psi hydrogen gas at 40° C. for 18 hours. Filter and concentrate to give the desired compound (802 mg).
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-f603027a811c4124b583d7961476ec7f |
| 出典メモ | uspto-grants-2010_06 |