関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenyl | HCID 11155794 | — |
| 反応物 | 1-(2-Chlorofuro[3,2-d]pyrimidin-4-yl)piperidine-4-carbonitrile | HCID 86665110 | — |
| 反応物 | HCID 178434350 | HCID 178434350 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | HCID 178434341 | HCID 178434341 | 28.2% |
反応手順
A mixture of K2CO3 (0.052 g, 0.38 mmol), Pd2dba3 (0.017 g, 0.019 mmol), 3-methyl-1H-indazol-6-amine (0.028 g, 0.19 mmol, Advanced ChemBlocks), 1-(2-chlorofuro[3,2-d]pyrimidin-4-yl)piperidine-4-carbonitrile (0.050 g, 0.19 mmol) and X-phos (0.018 g, 0.038 mmol) in 1,4-dioxane (10 mL) was stirred at about 100° C. for about 12 h. The solvent was removed and the residue was purified by Prep-TLC (DCM/MeOH 20:1) to give 1-(2-(3-methyl-1H-indazol-6-ylamino)furo[3,2-d]pyrimidin-4-yl)piperidine-4-carbonitrile (0.020 g, 28%): LC/MS (Table 2, Method 1) Rt=0.63 min; MS m/z: 374 (M+H)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08551981B2 |
|---|
| 出典データセット | uspto-grants-2013_10 |
|---|
| ORD ID | ord-b61ffce07c7042d59e42646d4ec6d385 |
|---|
| 出典メモ | uspto-grants-2013_10 |
|---|
