関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 1,2-Dimethoxyethane | HCID 8071 | — |
| 反応物 | Potassium Phosphate, Tribasic | HCID 62657 | — |
| 反応物 | 3-Aminophenylboronic acid hydrochloride | HCID 2763241 | — |
| 反応物 | 6-Bromo-8-(2-pyridin-4-yl-imidazol-1-yl)-imidazo[1,2-a]pyrazine | HCID 18440319 | — |
| 触媒 | Tetrakis(triphenylphosphine)palladium | HCID 11979704 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | 3-[6-Bromo-8-(2-pyridin-4-yl-imidazol-1-yl)-imidazo[1,2-a]pyrazin-6-yl]-phenylamine | HCID 18440317 | 66% |
反応手順
A mixture of 6-bromo-8-(2-pyridin-4-yl-imidazol-1-yl)-imidazo[1,2-a]pyrazine (4) (4.0 g), 3-aminophenylboronic acid hydrochloride (2.41 g), tetrakis(triphenylphosphine) palladium (Pd(PPh3)4) (1.36 g), 2.5 Maqueous potassium phosphate (K3PO3) (10 ml), and 1,2-dimethoxyethane (DME) (80 ml) is heated at 95° C. for 16 hours. The mixture is cooled to rt, treated with water (50 ml) and extracted with ethyl acetate (3×80 ml). The extracts are washed with water (1×50 ml) and brine (1×50 ml), dried over Na2SO4, and evaporated in vacuo. Purification on SiO2 (5% MeOH, DCM) yielded 3-[6 -Bromo-8-(2-pyridin-4-yl-imidazol-1-yl)-imidazo[1,2-a]pyrazin-6-yl]-phenylamine (5) (3.36 g) as a cream solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US07189723B2 |
|---|
| 出典データセット | uspto-grants-2007_03 |
|---|
| ORD ID | ord-00c6666bd043402199cb6618075b0413 |
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| 出典メモ | uspto-grants-2007_03 |
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