芳环上引入伯胺最常用的几种方法:硝基还原，Curtius重排反应及Hofmann降解反应等，这几种方法都是实验室很常用的方法。
本次分享的内容是铜催化芳基卤化物的伯胺化反应，卤素可为碘、溴；具体内容如下图所示
总结:该方法的底物适用范围比较广，适用于苯环类底物，也适用于吡啶环及五元杂环(噻吩)类底物；作者对比了不同氮源对反应产率的影响:浓氨水的反应效果比氯化铵好。
| A mixture of aryl bromide (1 mmol), ammonia (28%, 1 mL), CuI (38 mg, 0.2mmol), trans-4-hydroxy-L-proline (52.4 mg, 0.4mmol), and K2CO3 (414 mg, 3 mmol) in 2 mL of DMSO was heated at 50 °C until the bromide was consumed as monitored by TLC. The cooled mixture was partitioned between water and EA. The organic layer was separated, and the aqueous layer was extracted with EA. The combined organic layers were washed with brine, dried over Na2SO4, and concentrated in vacuo. The residue was purified by chromatography to provide the corresponding primaryaryl amine. |
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