Synthesis of 2,3,5-trisubstituted 1H-pyrroles via formal [3+2] cycloaddition of 1-arylpropynes and nitriles and their antiproliferative activities

被引：0

作者：

He, Dandan ^{[1
,2
,3
]}

Li, Ling ^{[1
,2
,3
]}

Wen, Xiong ^{[1
,2
,3
]}

Yin, Luxiang ^{[1
,2
,3
]}

Li, Jue ^{[1
,2
,3
]}

Wu, Sha ^{[1
,2
,3
]}

Li, Huili ^{[1
,2
,3
]}

Jiang, Fei ^{[1
,2
,3
]}

Shen, Xiangchun ^{[1
,2
,3
]}

机构：

[1] Guizhou Med Univ, Minist Educ, State Key Lab Funct & Applicat Med Plants, Key Lab Endem & Ethn Dis, 6 Ankang Ave & Guian New Dist, Guiyang 561113, Guizhou, Peoples R China

[2] Guizhou Med Univ, High Efficacy Applicat Nat Med Resources Engn Ctr, Key Lab Optimal Utilizat Nat Med Resources, 6 Ankang Ave & Guian New Dist, Guiyang 561113, Guizhou, Peoples R China

[3] Guizhou Med Univ, High Educ Key Lab Guizhou Prov Nat Med Pharmacol, 6 Ankang Ave & Guian New Dist, Guiyang 561113, Guizhou, Peoples R China

来源：

ORGANIC CHEMISTRY FRONTIERS | 2025年 / 12卷 / 04期

基金：

中国国家自然科学基金;

关键词：

ONE-POT SYNTHESIS; H BOND ADDITION; TETRASUBSTITUTED PYRROLES; REGIOSELECTIVE SYNTHESIS; DERIVATIVES; 2H-AZIRINES; ACCESS;

D O I：

10.1039/d4qo01999g

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A straightforward approach for the assembly of 2,3,5-trisubstituted 1H-pyrroles via a base-mediated [3 + 2] cycloaddition of 1-arylpropynes with nitriles has been reported through alkali metal salt-promoted C(sp3)-H functionalization. This reaction features a transition metal-free catalyst, facile starting materials and a wide substrate scope. Moreover, the biological evaluation revealed that these pyrrole products exhibit antiproliferative activities against MDA-MB-231, SGC-7901, and HCT-116 cells, which provides potential applications in pharmaceutical chemistry.

引用

页码：1150 / 1155

页数：6

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