Pd(II)/Cu(I) Co-catalyzed Dual C-H Functionalization of Indoles at C2 and C3 Positions Using Bifunctional Arylsulfonyl Reagents

被引：0
作者：
Huang, Jiahui [1 ,2 ,3 ]
Ai, Xiujuan [1 ,2 ,3 ]
Zhou, Shuai [1 ,2 ,3 ]
Li, Zixin [1 ,2 ,3 ]
Qi, Mengying [1 ,2 ,3 ]
You, Yuantao [1 ,2 ,3 ]
Yuan, Kedong [1 ,2 ,3 ]
机构：
[1] Guangzhou Med Univ, Guangzhou Municipal & Guangdong Prov Key Lab Mol T, NMPA, Guangzhou 511436, Peoples R China
[2] Guangzhou Med Univ, Sch Pharmaceut Sci, State Key Lab Resp Dis, Guangzhou 511436, Peoples R China
[3] Guangzhou Med Univ, Affiliated Hosp 5, Guangzhou 511436, Peoples R China
来源：
ORGANIC LETTERS | 2025年 / 27卷 / 21期
基金：
中国国家自然科学基金;
关键词：
REDUCTIVE ELIMINATION; PALLADIUM; ARYLATION; COMPLEXES; COPPER;
D O I：
10.1021/acs.orglett.5c01413
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A Pd(II)/Cu(I) co-catalyzed dual C-H functionalization strategy enables the one-pot synthesis of C2/C3-difunctionalized indoles using arylsulfonyl reagents. In this method, Cu(I) reduces S(VI) reagents to generate arylsulfonyl radicals, which react with Pd(II) to form electrophilic Ar-Pd(III) intermediates. These intermediates regioselectively arylate indoles at the C2 position, followed by Cu(II)-mediated C-H functionalization at the C3 position, to deliver the final products. This synergistic method enhances efficiency, reduces waste, and streamlines complex indole functionalization.
引用
收藏
页码：5440 / 5445
页数：6
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