関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Ethyl Acetate | HCID 8857 | — |
| 反応物 | Sodium Carbonate | HCID 10340 | — |
| 反応物 | 2-Amino-3-chloropyrazine | HCID 276224 | — |
| 反応物 | B-[6-(cyclohexyloxy)-3-pyridinyl]Boronic acid | HCID 66747855 | — |
| 触媒 | HCID 178418397 | HCID 178418397 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | 1,2-Dimethoxyethane | HCID 8071 | — |
| 生成物 | 3-[6-(Cyclohexyloxy)pyridin-3-yl]pyrazin-2-amine | HCID 66748561 | 79.6% |
反応手順
Tetrakis(triphenylphosphine)palladium(0) (53.5 mg) was added to a suspension of 3-chloropyrazin-2-amine (200 mg), 6-(cyclohexyloxy)pyridin-3-ylboronic acid (375 mg) and sodium carbonate (327 mg) in DME (5 mL) and water (1 mL) and the mixture was stirred at 90° C. under nitrogen for 3 hr. Water and EtOAc were added and the organic layer was separated, washed with brine, dried over anhydrous sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel, eluted with EtOAc in hexane) and washed with IPE to give the title compound (332 mg) as brown gum.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08778934B2 |
|---|
| 出典データセット | uspto-grants-2014_07 |
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| ORD ID | ord-3dd1162dd921459f977327b3ac0b5e49 |
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| 出典メモ | uspto-grants-2014_07 |
|---|
