Molecular Iodine-Catalysed Reductive Alkylation of Indoles: Late-Stage Diversification for Bioactive Molecules

被引：11

作者：

Cheng, Xionglve ^{[1
]}

Wang, Lili ^{[1
]}

Liu, Yide ^{[1
]}

Wan, Xiao ^{[1
]}

Xiang, Zixin ^{[1
]}

Li, Ruyi ^{[1
]}

Wan, Xiaobing ^{[1
]}

机构：

[1] Soochow Univ, Key Lab Organ Synth Jiangsu Prov, Coll Chem Chem Engn & Mat Sci, Suzhou 215123, Peoples R China

来源：

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY | 2022年 / 2022卷 / 34期

关键词：

Alkylation; Indoles; Metal-free; Reduction; Silanes; FRIEDEL-CRAFTS ALKYLATION; CARBONYL-COMPOUNDS; COUPLING REACTION; CASCADE REACTIONS; C-3; ALKYLATION; EFFICIENT; MILD; ALCOHOLS; HEXAFLUOROISOPROPANOL; HYDROSILANES;

D O I：

10.1002/ejoc.202200502

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Herein, we report a molecular iodine-catalysed reductive alkylation of indoles with carbonyl compounds using Et3SiH for the efficient synthesis of C3-alkylated indoles. This metal-free and environmental-friendly process exhibits excellent functional group tolerance, mild conditions, and wide substrate scope. Notably, the synthetic usefulness of this strategy to pharmacochemistry was highlighted by the late-stage modification of drug-like molecules.

引用

页数：5

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