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Diisopropylethylamine → Tert-Butyl (1S,3S,4S,5R)-3-{[(2S)-2-aminocarbonyl-1-pyrrolidinyl]carbonyl}-5-hydroxy-2-azabicyclo[2.2.2]octane-2-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | L-Prolinamide | HCID 111306 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | 1-Hydroxybenzotriazole hydrate | HCID 2796029 | — |
| 反応物 | (1S,3S,4S,5R)-2-tert-butoxycarbonyl-5-hydroxy-2-azabicyclo[2.2.2]octane-3-carboxylic acid | HCID 69135461 | — |
| 生成物 | Tert-Butyl (1S,3S,4S,5R)-3-{[(2S)-2-aminocarbonyl-1-pyrrolidinyl]carbonyl}-5-hydroxy-2-azabicyclo[2.2.2]octane-2-carboxylate | HCID 86598890 | — |
反応手順
To a solution of (1S,3S,4S,5R)-2-(tert-butoxycarbonyl)-5-hydroxy-2-azabicyclo[2.2.2]octane-3-carboxylic acid obtained in Example 2-5 (4.05 g), (2S)-2-pyrrolidinecarboxamide (1.77 g) and 1-hydroxybenzotriazole hydrate (1.68 g), were added 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (3.15 g) and N,N-diisopropylethylamine (5.2 mL) with cooling on an ice bath. After 5 minutes, the ice bath was removed and the mixture was stirred overnight at room temperature.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07186731B2 |
| 出典データセット | uspto-grants-2007_03 |
| ORD ID | ord-b2ab848cf9b44197b05f6964eb4950f0 |
| 出典メモ | uspto-grants-2007_03 |