参与物
| 角色 | 名称 | HCID | 投料 |
|---|
| 反应物 | 碳酸钾 | HCID 11430 | — |
| 反应物 | N,N-二甲基乙酰胺 | HCID 31374 | — |
| 反应物 | 1-Boc-4-氨基哌啶 | HCID 1268291 | — |
| 反应物 | 1-(6-Chloropyrimidin-4-yl)-5-(methylsulfonyl)indoline | HCID 59566526 | — |
| 溶剂 | Sodium chloride; water | HCID 57417360 | — |
| 产物 | 4-[6-(5-Methanesulfonyl-2,3-dihydro-indol-1-yl)-pyrimidin-4-ylamino]-piperidine-1-carboxylic acid tert-butyl ester | HCID 58074125 | — |
反应步骤
A mixture of 6a (0.4 g, 1.29 mmol), 4-amino-piperidine-1-carboxylic acid tert-butyl ester (0.4 g, 1.5 eq), DMA (5 mL) and potassium carbonate (0.4 g, 2.2 eq) was heated at 80° C. for 42 h. After allowing the reaction mixture to cool down to room temperature, 100 mL of brine was added and the mixture was extracted with ethyl acetate twice (100 mL and 30 mL). The combined extracts were washed with brine (2×50 mL), dried over magnesium sulfate and filtered. The solvent was removed under vacuum to give a solution of 6b in DMA.
来源与证据
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 专利号 | US08481731B2 |
|---|
| 来源数据集 | uspto-grants-2013_07 |
|---|
| ORD ID | ord-4a1b421ad8224d65bd9a3b41614f8ef6 |
|---|
| 来源说明 | uspto-grants-2013_07 |
|---|
