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Asymmetric macrocyclization enabled by Rh(Ⅲ)-catalyzed C-H activation:Enantioenriched macrocyclic inhibitor of Zika virus infection
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作者 Chao Chen Wenwen Yu +10 位作者 guangen huang Xuelian Ren Xiangli Chen Yixin Li Shenggui Liang Mengmeng Xu Mingyue Zheng Yaxi Yang He huang Wei Tang Bing Zhou 《Chinese Chemical Letters》 SCIE CAS 2024年第11期378-383,共6页
The development of enantioselective C-H macrocyclizations to efficiently access structurally diversified macrocycles is highly desirable,but remain a big challenge.Herein,we reported the first rhodium(Ⅲ)-catalyzed as... The development of enantioselective C-H macrocyclizations to efficiently access structurally diversified macrocycles is highly desirable,but remain a big challenge.Herein,we reported the first rhodium(Ⅲ)-catalyzed asymmetric intramolecular C-H macrocyclization,enabling the efficient synthesis of structurally diverse enantioenriched macrocycles.This robust enantioselective C-H macrocyclization has a broad functional group tolerance,excellent enantioselectivities(up to 98.5:1.5 e.r.)and a mild reaction condition,releasing CO_(2)as the single by-product.More significantly,the resulting unique enantioenriched19-membered macrocycle 2f was found to demonstrate a potent in vitro anti-Zika virus(ZIKV)activity without obvious cytotoxicity.Further investigation revealed that the anti-ZIKV activity is presumably attributed to an autophagy inhibition in the early stage of viral infection by down-regulating the expression of autophagy related gene Atg12. 展开更多
关键词 C-H activation Carboamidation Enantioselective macrocyclization Anti-Zika virus activity
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