関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 4-Fluoroiodobenzene | HCID 9605 | — |
| 反応物 | Potassium Phosphate, Tribasic | HCID 62657 | — |
| 反応物 | 1-N,2-N-dimethylcyclohexane-1,2-diamine | HCID 551074 | — |
| 反応物 | methyl 3-fluoro-1H-indole-6-carboxylate | HCID 59625843 | — |
| 触媒 | Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI) | HCID 24350 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | Methyl 3-fluoro-1-(4-fluorophenyl)-1H-indole-6-carboxylate | HCID 59625701 | — |
反応手順
Compound 21a (51 mg, 0.264 mmol), CuI (5 mg, 0.0264 mmol) and K3PO4 (40 mg, 0.66 mmol) were combined in a sealed reaction tube and the vial was back-flushed with N2. 4-Fluoro-iodobenzene 21b (0.0394 mL, 0.264 mmol) and N,N′-dimethylcyclohexane-1,2-diamine (0.0125 mL, 0.0792 mmol) were added via syringe, followed by toluene. The reaction mixture was heated at 95° C. for 6 h. The reaction was partitioned between EtOAc and water. The organic phase was concentrated and purified by flash column chromatography (silica gel, 20% EtOAc/hexanes) to give compound 21c.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08748417B2 |
|---|
| 出典データセット | uspto-grants-2014_06 |
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| ORD ID | ord-398a1f72757d400f8076e6663bf66744 |
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| 出典メモ | uspto-grants-2014_06 |
|---|
