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Sulfuric acid magnesium salt (1:1) → (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-N-(5-methoxyindol-3-yl-methyl)-4-piperidinamine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sulfuric acid magnesium salt (1:1) | HCID 24083 | — |
| 反応物 | 5-Methoxyindole-3-carbaldehyde | HCID 82758 | — |
| 反応物 | Sodium borohydride | HCID 4311764 | — |
| 反応物 | (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-4-piperidinamine | HCID 53839030 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-N-(5-methoxyindol-3-yl-methyl)-4-piperidinamine | HCID 57096920 | — |
反応手順
200 mg (0.551 mmol) of (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-4-piperidinamine are reacted in analogy to Example 2g with 116 mg (0.661 mmol) of 5-methoxyindole-3-carboxaldehyde and 90 mg of magnesium sulfate in 2 ml of toluene and subsequently reduced with 22 mg (0.584 mmol) of sodium borohydride in 2 ml of methanol. The title compound ##STR95## is obtained (98 mg, 34%) as white foam. TLC: methylene chloride/methanol/conc. ammonia (1000:50:1) Rf =0.42, FD-MS: M+ =521, 523. IR: 3460, 1630 cm-1.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05541195 |
| 出典データセット | uspto-grants-1996_07 |
| ORD ID | ord-120144aeb85c4ff99df5cafea6f46e72 |
| 出典メモ | uspto-grants-1996_07 |