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Benzylamine → 1-(1,1-dimethylethyl)-N-(phenylmethyl)-4-Piperidinamine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Benzylamine | HCID 7504 | — |
| 反応物 | 1-tert-Butyl-4-piperidone | HCID 73840 | — |
| 反応物 | Sodium triacetoxyborohydride | HCID 5049666 | — |
| 溶媒 | Acetic Acid | HCID 176 | — |
| 生成物 | 1-(1,1-dimethylethyl)-N-(phenylmethyl)-4-Piperidinamine | HCID 22647939 | 26.3% |
反応手順
A solution of 1-tert-butyl-4-oxopiperidine (3.6 g, 23.1), benzylamine (5.1 ml, 46.8 mmol), acetic acid (1.5 ml) and sodium triacetoxyborohydride (7.38 g, 34.8 mmol) was stirred at ambient for 2 days. Reaction mixture reduced in vacuo, residue partitioned between aqueous K2CO3 and EtOAc. The organic portion was dried (Na2SO4), filtered and reduced in vacuo. The residue was subjected to chromatography using CH2Cl2/MeOH/NH4OH (87/12/1) as the eluent to yield N-benzyl-1-tert-butylpiperidin-4-amine (1.5 g) (LC/MS: Rt 0.45, [M+H]+ 247).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08080666B2 |
| 出典データセット | uspto-grants-2011_12 |
| ORD ID | ord-49a1ebe5ca1e4759981e9da023f1486c |
| 出典メモ | uspto-grants-2011_12 |