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Potassium Phosphate, Tribasic → 4-{6-[3-(4-Fluorophenyl)-1-trityl-1H-4-pyrazolyl]imidazo[1,2-a]pyridin-3-yl}benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Phosphate, Tribasic | HCID 62657 | — |
| 反応物 | 4-(Tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide | HCID 2760588 | — |
| 反応物 | 6-[3-(4-fluorophenyl)-1-trityl-1H-pyrazolyl]-3-iodoimidazo[1,2-a]pyridine | HCID 22031070 | — |
| 触媒 | HCID 178418397 | HCID 178418397 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 4-{6-[3-(4-Fluorophenyl)-1-trityl-1H-4-pyrazolyl]imidazo[1,2-a]pyridin-3-yl}benzamide | HCID 22031498 | 43.2% |
反応手順
222 mg of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide prepared according to T. Ishiyama et al., J. Org. Chem., 60, 7508 (1995), 323 mg of 6-[3-(4-fluorophenyl)-1-trityl-1H-pyrazolyl]-3-iodoimidazo[1,2-a]pyridine (compound in Production Example 39), 200 mg tripotassium phosphate, 30 mg tetrakis(triphenylphosphine)palladium and 30 mL N,N-dimethylformamide were heated at 75° C. for 3 hours under nitrogen atmosphere. The solvent was removed, and the residue was purified by NH silica gel chromatography (hexane/ethyl acetate) to give 138 mg of the title compound (film).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07074801B1 |
| 出典データセット | uspto-grants-2006_07 |
| ORD ID | ord-beca258f008742348208e589e2ecd2f0 |
| 出典メモ | uspto-grants-2006_07 |