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4-[1-(4-Methoxybenzyl)amino-5-isoquinolyl]amino-1-(tert-butoxycarbonyl)piperidine → 4-(1-Amino-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-[1-(4-Methoxybenzyl)amino-5-isoquinolyl]amino-1-(tert-butoxycarbonyl)piperidine | HCID 21979935 | — |
| 溶媒 | Trifluoroacetic acid | HCID 6422 | — |
| 生成物 | 4-(1-Amino-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidine | HCID 21979787 | 99.6% |
反応手順
A solution of Intermediate 132 (270 mg) in 95% trifluoroacetic acid (5 ml) was stirred at 50° C. for 16 hours, and the solvent was evaporated under reduced pressure. The residue was added with dioxane (3 ml), 2 N aqueous sodium hydroxide (1 ml) and 2 di-t-butyl dicarbonate (393 mg) and stirred at room temperature for 1 hour. The solvent was evaporated under reduced pressure, and then the residue was purified by silica gel column chromatography (n-hexane:ethyl acetate:isopropylamine=5:5:1) to obtain the title compound (199 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07094789B2 |
| 出典データセット | uspto-grants-2006_08 |
| ORD ID | ord-b3e1fac3b5b54f7b92bfe077e81f3e7b |
| 出典メモ | uspto-grants-2006_08 |