関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Nitrogen | HCID 947 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 3-Amino-5-bromopyridine | HCID 817681 | — |
| 反応物 | 7-(4-Fluoro-phenyl)-imidazo[1,2-a]pyridine | HCID 59320799 | — |
| 触媒 | HCID 178418397 | HCID 178418397 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 5-[7-(4-Fluoro-phenyl)-imidazo[1,2-a]pyridin-3-yl]-pyridin-3-ylamine | HCID 59321107 | — |
反応手順
To 7-(4-fluoro-phenyl)-imidazo[1,2-a]pyridine (0.1093 g, 0.52 mmol) and 3-amino-5-bromopyridine (0.181 g, 1.05 mmol) in DMF (2 mL) was added 0.5 M K2CO3 (2.06 mL, 1.03 mmol). The reaction vessel was purged with N2 and Pd(PPh3)4 (63 mg, 0.055 mmol) added. The vessel was further purged with N2 and then heated in the microwave at 120° C. for 30 mins. Further 3-amino-5-bromopyridine (0.13 g, 0.75 mmol) and Pd(PPh3)4 (43 mg, 0.037 mmol) were added and the reaction heated in the microwave at 140° C. for 1 hour. The solids were filtered and the filtrate was concentrated in vacuo. The residue was partitioned between H2O (20 ml) and EtOAc (2×20 mL). The combined organic phases were dried over MgSO4, filtered and concentrated in vacuo and the product used crude in the subsequent reaction.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08895745B2 |
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| 出典データセット | uspto-grants-2014_11 |
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| ORD ID | ord-d0fec6e4f8084c1d8ebd539e025d9d5e |
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| 出典メモ | uspto-grants-2014_11 |
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