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HRID 916361作成日：2026年10月26日
1,8-Diazabicyclo(5.4.0)undec-7-ene → [1-(4-Cyanonaphthalen-1-yl)piperidin-3-ylmethyl]carbamic acid tert-butyl ester
https://huagongshe.com/reaction/916361
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 1,8-Diazabicyclo(5.4.0)undec-7-ene | HCID 81184 | — |
| 反応物 | 1-Cyano-4-fluoronaphthalene | HCID 2736734 | — |
| 反応物 | tert-butyl N-[(piperidin-3-yl)methyl]carbamate | HCID 2756030 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | [1-(4-Cyanonaphthalen-1-yl)piperidin-3-ylmethyl]carbamic acid tert-butyl ester | HCID 69224037 | 71.1% |
反応手順
1-Cyano-4-fluoronaphthalene (273 mg, 1.60 mmol), tert-butyl (piperidin-3-ylmethyl)carbamate (411 mg, 1.92 mmol) and DBU (25 μl, 0.16 mmol) were dissolved in pyridine (4 mL) and stirred at 60° C. for 4 days. The reaction was worked up in the same way as for 198RL60 followed by purification using silica gel column chromatography eluted with a stepwise gradient of 0-70% ethyl acetate in n-heptane, giving the desired compound (416 mg, 71%) as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07268232B2 |
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| 出典データセット | uspto-grants-2007_09 |
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| ORD ID | ord-b200cc29be814ade8c3414993330c44d |
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| 出典メモ | uspto-grants-2007_09 |
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