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Ethyl 4-cyclohexyl-2-oxobutanoate → benzyl 3(S)-[1(R)-ethoxycarbonyl-3-cyclohexylpropyl]amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-5-acetate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ethyl 4-cyclohexyl-2-oxobutanoate | HCID 13454680 | — |
| 反応物 | benzyl 3(S)-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-5-acetate hydrochloride | HCID 18599732 | — |
| 生成物 | benzyl 3(S)-[1(R)-ethoxycarbonyl-3-cyclohexylpropyl]amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-5-acetate | HCID 70046892 | 18.5% |
反応手順
Benzyl 3(S)-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-5-acetate hydrochloride (1.5 g) and ethyl 4-cyclohexyl-2-oxobutyrate (2.63 g) are subjected to reductive alkylation reaction in a manner similar to that described in Example 16, and the product is purified by silica gel column chromatography (hexane:ethal acetate=5:1-4:1). From the first fraction, 0.4 g of benzyl 3(S)-[1(R)-ethoxycarbonyl-3-cyclohexylpropyl]amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-5-acetate is obtained as a colorless oil.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US04548932 |
| 出典データセット | uspto-grants-1985_10 |
| ORD ID | ord-e588394232fc485292af739d6142339c |
| 出典メモ | uspto-grants-1985_10 |