関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Binap, (A+-)- | HCID 634876 | — |
| 反応物 | 1-Allylpiperazine | HCID 806422 | — |
| 反応物 | 4-Isopropyl-benzenesulfonic acid 6-chloro-pyridin-3-yl ester | HCID 86606504 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | HCID 54674950 | HCID 54674950 | 21% |
反応手順
A flask containing 45 mg of palladium(II) acetate (0.2 mmol), 126 mg of BINAP (0.20 mmol) and 0.233 mg of sodium tert-butylate in dry toluene (15 mL) was flushed with nitrogen 1.275 g of 1-allylpiperazin (10 mmol) were added and the reaction mixture was heated to 50° C. 630 mg of 4-isopropyl-benzenesulfonic acid 6-chloro-pyridin-3-yl ester (2.0 mmol) were dissolved in toluene and the solution was slowly added over a period of 10 minutes into the reaction mixture with stirring. The mixture was heated to reflux with stirring for 7 h. Thereby 4-isopropyl-benzenesulfonic acid 6-(4-allyl-piperazin-1-yl)-pyridin-3-yl ester was obtained in 21% yield.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08476275B2 |
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| 出典データセット | uspto-grants-2013_07 |
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| ORD ID | ord-2509701e99e1458488d8496679cb9a01 |
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| 出典メモ | uspto-grants-2013_07 |
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