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Cesium carbonate → 2-[3-(3-Fluoro-4-morpholin-4-yl-piperidin-1-yl)-phenyl]-1-methyl-1H-benzoimidazole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | Binap, (A+-)- | HCID 634876 | — |
| 反応物 | 2-(3-bromophenyl)-1-methyl-1H-benzimidazole | HCID 962451 | — |
| 反応物 | 4-(3-Fluoro-piperidin-4-yl)-morpholine | HCID 68670746 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | 2-[3-(3-Fluoro-4-morpholin-4-yl-piperidin-1-yl)-phenyl]-1-methyl-1H-benzoimidazole | HCID 68671327 | — |
反応手順
4-(3-Fluoro-piperidin-4-yl)-morpholine (0.085 g, 0.45 mmol), 2-(3-Bromo-phenyl)-1-methyl-1H-benzoimidazole (described in method N, step a, b) (0.10 g, 0.35 mmol), and cesium carbonate (10.50 g, 32.2 mmol) were placed into a dry sealed 7 mL vial under nitrogen and dry toluene (0.4 mL) was added. At the same time Palladium acetate (0.016 g, 0.07 mmol), and BINAP (0.065 g, 0.10 mmol) were placed into another dry sealed 7 mL vial under nitrogen and diluted with dry toluene (0.8 mL) After about 20 minutes the resulting suspension was added to the vial containing the starting materials.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08592463B2 |
| 出典データセット | uspto-grants-2013_11 |
| ORD ID | ord-639d0b6d540e4f4bafe23bf639e62468 |
| 出典メモ | uspto-grants-2013_11 |