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钯催化2-卤代-Boc-芳基苯甲酰胺的分子内C-H芳基化反应用于合成N-H菲啶酮。

Palladium-catalyzed intramolecular C-H arylation of 2-halo--Boc--arylbenzamides for the synthesis of N-H phenanthridinones.

作者信息

Hu Quan-Fang, Gao Tian-Tao, Shi Yao-Jie, Lei Qian, Yu Luo-Ting

机构信息

State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University and Collaborative Innovation Center Chengdu 610041 China

出版信息

RSC Adv. 2018 Apr 13;8(25):13879-13890. doi: 10.1039/c8ra02099j. eCollection 2018 Apr 11.

Abstract

A palladium catalyzed synthesis of N-H phenanthridinones was developed C-H arylation. The protocol gives phenanthridinones regioselectively by one-pot reaction without deprotection. It exhibits broad substrate scope and affords targets in up to 95% yields. Importantly, it could be applied for the less reactive -chlorobenzamides.

摘要

开发了一种钯催化的通过C-H芳基化合成N-H菲啶酮的方法。该方案通过一锅反应区域选择性地得到菲啶酮,无需脱保护。它具有广泛的底物范围,产率高达95%。重要的是,它可应用于活性较低的氯代苯甲酰胺。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/314d/9079793/8e0509a16f77/c8ra02099j-s1.jpg

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