Direct Palladium-Catalyzed β-Arylation of Lactams

被引：28
作者：
Chen, Ming [1 ]
Liu, Feipeng [1 ,2 ]
Dong, Guangbin [1 ]
机构：
[1] Univ Chicago, Dept Chem, Chicago, IL 60637 USA
[2] China Agr Univ, Dept Appl Chem, 2 West Yuanmingyuan Rd, Beijing 100193, Peoples R China
来源：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2018年 / 57卷 / 14期
关键词：
C-H activation; heterocylces; lactams; palladium; reaction mechanisms; C-H BONDS; ALPHA-AMINO-ACIDS; UNACTIVATED C(SP(3))-H BONDS; CARBON-HYDROGEN BONDS; INTERMOLECULAR ARYLATION; ASYMMETRIC ARYLATION; REMOVABLE AUXILIARY; ARYL BROMIDES; LIGAND; FUNCTIONALIZATION;
D O I：
10.1002/anie.201800958
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A direct and catalytic method is reported here for -arylation of N-protected lactams with simple aryl iodides. The transformation is enabled by merging soft enolization of lactams, palladium-catalyzed desaturation, Ar-X bond activation, and aryl conjugate addition. The reaction is operated under mild reaction conditions, is scalable, and is chemoselective. Application of this method to concise syntheses of pharmaceutically relevant compounds is demonstrated.
引用
收藏
页码：3815 / 3819
页数：5
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