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Hydrochloric Acid → 3-(piperidin-4-yl)-1,6-naphthyridin-2(1H)-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Hydrochloric Acid | HCID 313 | — |
| 反応物 | tert-Butyl 4-(1-hydroxy-3-methoxy-3-oxo-1-(4-pivalamidopyridin-3-yl)propan-2-yl)piperidine-1-carboxylate | HCID 59732007 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | 3-(piperidin-4-yl)-1,6-naphthyridin-2(1H)-one | HCID 59731944 | 77% |
反応手順
Concentrated hydrochloric acid (8.0 mL, 97 mmol) was added with stirring to a mixture of tert-butyl 4-(1-hydroxy-3-methoxy-3-oxo-1-(4-pivalamidopyridin-3-yl)propan-2-yl)piperidine-1-carboxylate (1.2 g, 2.6 mmol) and water (24 mL). Reaction was heated to reflux and held for 14 hours. Mixture was concentrated in vacuo. Residue was treated with acetonitrile (70 mL) and then concentrated in vacuo. Residue was crystallized from ethanol. Title compound was obtained as white solid in 77% yield. (M+H)+=230.1.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07384930B2 |
| 出典データセット | uspto-grants-2008_06 |
| ORD ID | ord-948e54cfa62a4ae8bf8c4150001aeecf |
| 出典メモ | uspto-grants-2008_06 |