Synthesis of C3-Alkylated Indoles on DNA via Indolyl Alcohol Formation Followed by Metal-Free Transfer Hydrogenation

被引：22

作者：

Cai, Pinwen ^{[1
]}

Yang, Guanyu ^{[1
]}

Zhao, Lanzhou ^{[1
]}

Wan, Jinqiao ^{[1
]}

Li, Jin ^{[1
]}

Liu, Guansai ^{[1
]}

机构：

[1] HitGen Inc, Discovery Chem Unit, Bldg 6,8 Huigu 1st East Rd, Chengdu 610200, Sichuan, Peoples R China

来源：

ORGANIC LETTERS | 2019年 / 21卷 / 17期

关键词：

ENCODED CHEMICAL LIBRARIES; INHIBITORS; 2-ARYLINDOLES; TECHNOLOGY; DIVERSITY; CHEMISTRY; POTENT;

D O I：

10.1021/acs.orglett.9b02132

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

3-Alkylated indole cores have been found in countless natural products and many biologically active compounds, including pharmaceuticals. In this report, a highly efficient approach to C3-alkylated indole derivatives on DNA via indolyl alcohol formation followed by metal-free transfer hydrogenation is developed. This on-DNA C3 alkylation approach is attractive because library compounds can be constructed from simple aldehydes or acid functionalized aldehydes, which are widely commercially available.

引用

页码：6633 / 6637

页数：5

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