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A Catalyst-Free Synthesis of Fused Perfluoroalkylated 2,3-Dihydroisoxazoles via Oxa-Michael-Aldol Annulation
Synthesis ( IF 2.6 ) Pub Date : 2021-08-31 , DOI: 10.1055/a-1625-9538
Wei Zhou 1 , Lan Yao 2 , Yongxiurong Liu 1 , Lichun Shen 1 , Jie Chen 1 , Hongmei Deng 1 , Min Shao 3 , Hui Zhang 4 , Xiaojun Tang 1 , Weiguo Cao 1
Affiliation  

A novel synthesis of fused perfluoroalkylated 2,3-dihydroisoxazoles is achieved via oxa-Michael-aldol annulation between perfluoroalk-2-ynoates and N-hydroxyimides. This method provides a convenient route for the synthesis of pyrrolidin-2-one-fused perfluoroalkylated 2,3-dihydroisoxazoles in yields of up to 97%. Diverse and pharmaceutically attractive polycyclic scaffolds can be obtained rapidly and efficiently under these mild, catalyst-free conditions.

中文翻译:

通过 Oxa-Michael-Aldol 环化无催化剂合成稠合全氟烷基化 2,3-二氢异恶唑

稠合全氟烷基化 2,3-二氢异恶唑的新合成是通过全氟烷-2-炔酸酯和 N-羟基酰亚胺之间的氧杂-迈克尔-羟醛环化实现的。该方法为合成吡咯烷-2-一个-稠合的全氟烷基化 2,3-二氢异恶唑提供了一条便捷的途径,产率高达 97%。在这些温和、无催化剂的条件下,可以快速有效地获得多样化且具有药学吸引力的多环支架。
更新日期:2021-09-19
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