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HRID 336388作成日：2026年10月26日
(4-Fluoro-3-methylphenyl)boronic acid → 2-(3-(4-Fluoro-3-methyl-phenyl)-5-phenyl-(1,2,4)triazol-1-yl)-1-(4-pyrimidin-2-yl-piperazin-1-yl)-ethanone
https://huagongshe.com/reaction/336388
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | (4-Fluoro-3-methylphenyl)boronic acid | HCID 2774580 | — |
| 反応物 | Sodium dicarbonate | HCID 22718997 | — |
| 反応物 | 2-(3-Bromo-5-phenyl-(1,2,4)triazol-1-yl)-1-(4-pyrimidin-2-yl-piperazin-1-yl)-ethanone | HCID 86690171 | — |
| 触媒 | HCID 178418397 | HCID 178418397 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 2-(3-(4-Fluoro-3-methyl-phenyl)-5-phenyl-(1,2,4)triazol-1-yl)-1-(4-pyrimidin-2-yl-piperazin-1-yl)-ethanone | HCID 71612649 | 30% |
反応手順
15 mg tetrakis(triphenylphosphine)palladium(0) was added to 100 mg 2-(3-bromo-5-phenyl-(1,2,4)triazol-1-yl)-1-(4-pyrimidin-2-yl-piperazin-1-yl)-ethanone, 500 μL 2 mol/L aqueous sodiumdicarbonate solution and 43 mg 4-fluoro-3-methylphenylboronic acid in 10 mL dioxane under nitrogen. The reaction was stirred over night at 120° C. The reaction was filltered and evaporated. The residue was purified by HPLC to give 32 mg of the desired product.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08889677B2 |
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| 出典データセット | uspto-grants-2014_11 |
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| ORD ID | ord-84aea2a5210d410c990142fca04841a1 |
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| 出典メモ | uspto-grants-2014_11 |
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