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HRID 32161作成日：2026年10月24日
Potassium Phosphate, Tribasic → (R)-1-butyl-4-[2-(4,4-dimethylcyclohexyl)-4-(3-methoxypiperidin-1-yl)phenyl]piperazine
https://huagongshe.com/ja/reaction/32161
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Potassium Phosphate, Tribasic | HCID 62657 | — |
| 反応物 | Tri-tert-butylphosphine tetrafluoroborate | HCID 2734635 | — |
| 反応物 | 1-[4-Bromo-2-(4,4-dimethylcyclohexyl)phenyl]-4-butylpiperazine | HCID 23141738 | — |
| 反応物 | (3R)-3-methoxypiperidine hydrochloride | HCID 69216666 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 溶媒 | O-Xylene | HCID 7237 | — |
| 生成物 | (R)-1-butyl-4-[2-(4,4-dimethylcyclohexyl)-4-(3-methoxypiperidin-1-yl)phenyl]piperazine | HCID 59769385 | 59.2% |
反応手順
A mixture of 1-[4-bromo-2-(4,4-dimethylcyclohexyl)phenyl]-4-butylpiperazine (37.4 mg, 0.0918 mmol) produced in Example (21c), (R)-3-methoxypiperidine hydrochloride (16.7 mg, 0.110 mmol) produced in Example (49a), tripotassium phosphate (170 mg, 0.801 mmol), palladium(II) acetate (8.2 mg, 0.0365 mmol), tri-t-butylphosphonium tetrafluoroborate (32 mg, 0.110 mmol) and xylene (1.5 mL) was stirred for 4 hours and 30 minutes at an external temperature of 100° C. under a nitrogen atmosphere. The mixture was air-cooled to room temperature and then purified by NH silica gel column chromatography (ethyl acetate/hexane) to give 24 mg of (R)-1-butyl-4-[2-(4,4-dimethylcyclohexyl)-4-(3-methoxypiperidin-1-yl)phenyl]piperazine as a colorless oil.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US07425554B2 |
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| 出典データセット | uspto-grants-2008_09 |
|---|
| ORD ID | ord-1059d9599d9f45f89d302d12e19044cb |
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| 出典メモ | uspto-grants-2008_09 |
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