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Succinic anhydride → 4-[((1S,2R)-1-(3,5-difluorobenzyl)-3-{[1-(3-ethylphenyl)cyclopropyl)amino}-2-hydroxypropyl)amino]-4-oxobutanoic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Succinic anhydride | HCID 7922 | — |
| 反応物 | 3-Amino-4-(3,5-difluoro-phenyl)-1-[1-(3-ethyl-phenyl)-cyclopropylamino]-butan-2-ol | HCID 21085482 | — |
| 溶媒 | Chloroform | HCID 6212 | — |
| 生成物 | 4-[((1S,2R)-1-(3,5-difluorobenzyl)-3-{[1-(3-ethylphenyl)cyclopropyl)amino}-2-hydroxypropyl)amino]-4-oxobutanoic acid | HCID 57512111 | — |
反応手順
To a solution of 3-Amino-4-(3,5-difluoro-phenyl)-1-[1-(3-ethyl-phenyl)-cyclopropylamino]-butan-2-ol (0.500 g, 1.387 mmol) in chloroform (7 ml) was added TEA (0.58 ml, 4.161 mmol) with stirring under nitrogen for 30 min. To this solution was added succinic anhydride (0.138 g, 1.387 mmol) and reaction was stirred overnight at 50° C. The next morning reaction mixture was concentrated in vacuo, yielding the product. (ES+: 461.2)
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07727997B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-4a032367bbd647bf9b5da8cedcc1a131 |
| 出典メモ | uspto-grants-2010_06 |