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HRID 456422作成日:2026年10月26日
Diisopropylethylamine → (R)-2-[6-(4-Trifluoromethyl-phenyl)-pyridazin-3-yl]-octahydro-pyrido[1,2-a]pyrazine
https://huagongshe.com/reaction/456422
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | Tetrafluoro-m-phenylenediamine dihydrochloride | HCID 149026 | — |
| 反応物 | (R)-Octahydro-pyrido[1,2-a]pyrazine | HCID 773775 | — |
| 反応物 | Pyridazine, 3-chloro-6-[4-(trifluoromethyl)phenyl]- | HCID 12449554 | — |
| 溶媒 | Dimethyl Sulfoxide | HCID 679 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | (R)-2-[6-(4-Trifluoromethyl-phenyl)-pyridazin-3-yl]-octahydro-pyrido[1,2-a]pyrazine | HCID 20799063 | 98.1% |
反応手順
A mixture of the dihydrochloride salt of (R)-octahydropyrido[1,2-a]pyrazine (649 mg, 3.05 mmol), diisopropylethylamine (1.17 ml, 6.72 mmol), 3-chloro-6-(4-trifluoromethylphenyl)-pyridazine (290 mg, 1.12 mmol) and dimethylsulfoxide (1 ml) was heated in a closed vessel at 160° C. for 40 min. The reaction mixture was cooled to room temperature, diluted with dichloromethane (10 ml) and washed with water (2×15 ml) and brine (15 ml). The organic layer was dried over magnesium sulphate. The solvent was removed in vacuo to give 398 mg of the title compound as the free base.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07186721B2 |
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| 出典データセット | uspto-grants-2007_03 |
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| ORD ID | ord-bfd189a0842d47fd8b77df7eb5d727b1 |
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| 出典メモ | uspto-grants-2007_03 |
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