関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Pyrazole | HCID 1048 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | tert-Butyl 3-iodobenzylcarbamate | HCID 11645663 | — |
| 反応物 | (1S,2S)-(+)-N,N'-Dimethylcyclohexane-1,2-diamine | HCID 13822957 | — |
| 触媒 | Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI) | HCID 24350 | — |
| 溶媒 | Dimethyl Sulfoxide | HCID 679 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | tert-butyl-3-(1H-pyrazol-1-yl)benzylcarbamate | HCID 56791985 | 70.3% |
反応手順
To a solution of tert-butyl-3-iodobenzylcarbamate (550 mg, 1.65 mmol) in Dioxane (1.2 mL) and DMSO (1.2 mL) was added CuI (16 mg, 0.083 mmol), (1S,2S)—N1,N2-dimethylcyclohexane-1,2-diamine (0.052 ml, 0.33 mmol), pyrazole (135 mg, 1.98 mmol) and K2CO3 (479 mg, 3.47 mmol). After stirring at 120° C. for 3 h, it was concentrated and the residue was purified by column chromatography to give tert-butyl-3-(1H-pyrazol-1-yl)benzylcarbamate (317 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US09102625B2 |
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| 出典データセット | uspto-grants-2015_08 |
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| ORD ID | ord-953510000c43469085ac5217a1dfbbdd |
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| 出典メモ | uspto-grants-2015_08 |
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