関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 2,4-Dichloro-1,3,5-triazine | HCID 17810 | — |
| 反応物 | 5-(Methanesulfonyl)-2,3-dihydro-1H-indole | HCID 2736136 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 触媒 | Binap, (A+-)- | HCID 634876 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 1-(4-Chloro-[1,3,5]-triazin-2-yl)-5-methanesulfonyl-2,3-dihydro-1H-indole | HCID 86650175 | 83.7% |
反応手順
5-Methanesulfonyl-2,3-dihydro-1H-indole (79 mg, 0.4 mmol) was dissolved in dioxane (2 mL). 2,4-Dichloro-[1,3,5]-triazine (60 mg, 1 eq), palladium acetate (11 mg, 5% molar), (+/−)binap (15 mg, 8% molar) and cesium carbonate (131 mg, 1 eq) were added and the reaction mixture was heated at 100° C. for 4 h. The mixture was cooled to room temperature and water was added. The mixture was filtered through celite and washed three times with dioxane. The collected filtrate was evaporated to dryness to give 11a (104 mg) which was used for the next step without further purification.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08481731B2 |
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| 出典データセット | uspto-grants-2013_07 |
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| ORD ID | ord-c6be3730c18143329c854589768305da |
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| 出典メモ | uspto-grants-2013_07 |
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