Diastereoselective Formal [3+3] Cascade Cyclization towards Fused 4‐Fluoroalkylated 3,4‐Dihydro‐2H‐pyrans via Copper Catalysis DOI

Weigao Hu,

Jiawen Yin,

Zhiyong Li

и другие.

Chinese Journal of Chemistry, Год журнала: 2025, Номер unknown

Опубликована: Апрель 25, 2025

Comprehensive Summary The cycloaddition and annulation reactions offer a powerful method toward various important substituted 3,4‐dihydro‐2 H ‐pyran architectures. Nevertheless, the transformation for preparing fused‐polycyclic ones still remains challenging yet highly desirable until now. Herein, we report novel formal [3+3] cascade cyclization reaction to provide lactam‐fused 4‐fluoroalkylated 3,4‐dihydropyran skeletons bearing three contiguous tertiary carbon centers via copper catalysis. Of note, these annulations proceeded in an exclusively diastereoselective manner through successive inert C(sp 2 )‐Cl 3 )‐H functionalization, which exhibited site‐selectivity stereoselectivity. Additionally, evaluations on biological activities of obtained products revealed that several display inhibitory activity against Siha H1975 cancer cell lines.

Язык: Английский

Diastereoselective Formal [3+3] Cascade Cyclization towards Fused 4‐Fluoroalkylated 3,4‐Dihydro‐2H‐pyrans via Copper Catalysis DOI

Weigao Hu,

Jiawen Yin,

Zhiyong Li

и другие.

Chinese Journal of Chemistry, Год журнала: 2025, Номер unknown

Опубликована: Апрель 25, 2025

Comprehensive Summary The cycloaddition and annulation reactions offer a powerful method toward various important substituted 3,4‐dihydro‐2 H ‐pyran architectures. Nevertheless, the transformation for preparing fused‐polycyclic ones still remains challenging yet highly desirable until now. Herein, we report novel formal [3+3] cascade cyclization reaction to provide lactam‐fused 4‐fluoroalkylated 3,4‐dihydropyran skeletons bearing three contiguous tertiary carbon centers via copper catalysis. Of note, these annulations proceeded in an exclusively diastereoselective manner through successive inert C(sp 2 )‐Cl 3 )‐H functionalization, which exhibited site‐selectivity stereoselectivity. Additionally, evaluations on biological activities of obtained products revealed that several display inhibitory activity against Siha H1975 cancer cell lines.

Язык: Английский

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