関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | (Pyrimidin-5-yl)boronic acid | HCID 2795193 | — |
| 反応物 | 1-(3-Bromophenyl)-4-fluoro-1-(2-methoxypyridin-4-yl)-1H-isoindol-3-amine | HCID 58579498 | — |
| 触媒 | Bis(cyclopenta-1,4-dien-1-yl(diphenyl)phosphane);dichloropalladium;iron(2+) | HCID 178418228 | — |
| 溶媒 | Dimethoxyethane ethanol water | HCID 86587095 | — |
| 生成物 | 4-Fluoro-1-(2-methoxypyridin-4-yl)-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine | HCID 46206977 | 54% |
反応手順
1-(3-Bromophenyl)-4-fluoro-1-(2-methoxypyridin-4-yl)-1H-isoindol-3-amine (100 mg, 0.24 mmol), 5-pyrimidinylboronic acid (31.6 mg, 0.25 mmol), [1,1′-bis (diphenylphosphino)ferrocene]palladium(II) chloride (9.90 mg, 0.01 mmol), cesium carbonate (0.058 mL, 0.73 mmol) and DME:EtOH:water (6:3:1) (3.00 mL) were mixed in a microwave vial and heated in a microwave reactor at 150° C. for 20 min. The resulting product mixture was filtered and purified by preparative-HPLC to give 58 mg (54% yield of the title compound (after pooling and freeze drying of the fractions).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08030500B2 |
|---|
| 出典データセット | uspto-grants-2011_10 |
|---|
| ORD ID | ord-9e1f968b48c1411d928475e072084f6e |
|---|
| 出典メモ | uspto-grants-2011_10 |
|---|
