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Piperidine → (4-Isopropyl-piperazin-1-yl)-(5-piperidin-1-ylmethylpyrazin-2-yl)-methanone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Piperidine | HCID 8082 | — |
| 反応物 | Sodium triacetoxyborohydride | HCID 5049666 | — |
| 反応物 | Methyl 5-formylpyrazine-2-carboxylate | HCID 44515461 | — |
| 反応物 | 5-Piperidin-1-ylmethyl-pyrazine-2-carboxylic acid methyl ester | HCID 44515772 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | (4-Isopropyl-piperazin-1-yl)-(5-piperidin-1-ylmethylpyrazin-2-yl)-methanone | HCID 11544498 | 23% |
反応手順
5-Piperidin-1-ylmethyl-pyrazine-2-carboxylic acid methyl ester. A mixture of 5-formyl-pyrazine-2-carboxylic acid methyl ester (0.400 g, 2.40 mmol), piperidine (0.204 g, 2.40 mmol), and NaB(OAc)3H (1.40 g, 3.60 mmol) in DCM (10 mL) was stirred for 18 h at rt. The reaction was quenched by the addition of 10% aq. NaOH (10 mL) and the mixture was stirred for 30 min. The mixture was extracted with DCM (3×20 mL). The combined organic extracts were dried over Na2SO4, filtered, and concentrated to yield the title compound (0.130 g, 23%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07947718B2 |
| 出典データセット | uspto-grants-2011_05 |
| ORD ID | ord-0b6bdcabb8e64553bf4cfa5ac1e27b03 |
| 出典メモ | uspto-grants-2011_05 |