Palladium-Catalyzed Remote C(sp3)-H Arylation of 3-Pinanamine
Palladium-Catalyzed Remote C(sp3)-H Arylation of 3-Pinanamine
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DOI：
10.1021/ol502011k
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发表时间：
2014-08-15
期刊：
影响因子：
5.2
通讯作者：
Wang, Honggen
中科院分区：
文献类型：
--
作者：
Cui, Wei;Chen, Shengwei;Wang, Honggen
3-蒎烷胺是药物化学和不对称合成中常用的基序。为了寻求新型的基于3-频哪胺的抗流感病毒A剂，通过使用Pd催化的C（sp（3））-H活化逻辑实现了3-频哪胺的直接官能化。观察到良好的底物范围和官能团耐受性。该反应代表了脂肪胺在远端δ位置直接官能化的罕见实例。
3-Pinanamine is a prevalent motif in medicinal chemistry and asymmetric synthesis. In line with the pursuit of novel 3-pinanamine based anti-influenza virus A agent, the direct functionalization of 3-pinanamine was achieved by using Pd-catalyzed C(sp(3))-H activation logic. Good substrate scope and functional group tolerance were observed. The reaction represents a rare example of a direct functionalization of an aliphatic amine at the remote delta position.