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3-氨基喹啉 → 1-(5-Cyano-3-fluoro-6-(quinolin-3-ylamino)pyridin-2-ylamino)cyclopentanecarboxamide
参与物
| 角色 | 名称 | HCID | 投料 |
|---|---|---|---|
| 反应物 | 3-氨基喹啉 | HCID 11375 | — |
| 反应物 | 4,5-双二苯基膦-9,9-二甲基氧杂蒽 | HCID 636044 | — |
| 反应物 | 苯酚钠 | HCID 23681143 | — |
| 反应物 | 1-(6-Chloro-5-cyano-3-fluoropyridin-2-ylamino)cyclopentanecarboxamide | HCID 86666167 | — |
| 催化剂 | 三(二亚苄基丙酮)二钯 | HCID 9811564 | — |
| 溶剂 | 1,4-二氧六环 | HCID 31275 | — |
| 产物 | 1-(5-Cyano-3-fluoro-6-(quinolin-3-ylamino)pyridin-2-ylamino)cyclopentanecarboxamide | HCID 67509781 | — |
反应步骤
A mixture of 1-(6-chloro-5-cyano-3-fluoropyridin-2-ylamino)cyclopentanecarboxamide (90 mg, 0.318 mmol), 3-aminoquinoline (58 mg, 0.402 mmol), sodium phenoxide trihydrate (85 mg, 0.500 mmol), xantphos (30 mg, 0.051 mmol) and Pd2 dba3 (20 mg, 0.021 mmol) in dioxane (2 mL) was degassed with Ar, then was stirred at 110 C for 4 h. Water and EtOAc were added. The organic phase was washed with aq. 1N NaOH, dried over Na2SO4, concentrated in vacuo to give crude 1-(5-cyano-3-fluoro-6-(quinolin-3-ylamino)pyridin-2-ylamino)cyclopentanecarboxamide.
来源与证据
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 专利号 | US08846928B2 |
| 来源数据集 | uspto-grants-2014_09 |
| ORD ID | ord-32c07895909e4870bbc7b369a156f02c |
| 来源说明 | uspto-grants-2014_09 |