Natural carbolines inspired the discovery of chiral CarOx ligands for asymmetric synthesis and antifungal leads
Natural carbolines inspired the discovery of chiral CarOx ligands for asymmetric synthesis and antifungal leads
复制标题
天然咔啉启发了用于不对称合成和抗真菌先导化合物的手性 CarOx 配体的发现
DOI：
10.1039/d0qo00519c
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发表时间：
2020-08-21
影响因子：
5.4
通讯作者：
Li, Shengkun
中科院分区：
文献类型：
--
作者：
Lai, Jixing;Li, Wei;Li, Shengkun
通过alangiobussinine和特权的吡啶-恶唑啉支架的杂交，构思了前所未有的β-CarOx配体。他们表现良好，在高对映选择性的Pd催化的迈克尔加成芳基硼酸硝基苯乙烯和β-取代的环烯酮（高达99%ee）。与alangiobussinine相比，β-CarOx配体也显示出增强的抗真菌作用，证明了对核盘菌有希望的抗真菌线索。
The unprecedented beta-CarOxligands were conceived by the hybridization of alangiobussinine and the privileged pyridine-oxazoline scaffold. They performed well in the highly enantioselective Pd-catalyzed Michael addition of arylboronic acids to nitrostyrenes and beta-substituted cyclic enone (up to 99% ee). The beta-CarOxligands also showed an enhanced antifungal effect compared to alangiobussinine, demonstrating promising antifungal leads againstSclerotinia sclerotiorum.