Protecting-group-free enantioselective tandem allylic substitution of o-phenylenediamines and o-aminophenols

Green Synthesis and Catalysis

Jerome Claverie¹  Jicheng Shi²  Wenjun Tang³  Xuehua Kang⁴  Chao Qian⁵  He Yang⁵ 

[1] Corresponding authors.;College of Chemistry, Maoming Technology Center of Organic Materials, Guangdong University of Petrochemical Technology, Maoming 525000, China;Department of Chemistry, University of Sherbrooke, Sherbrooke J1K2R1, Canada;School of Physical Science and Technology, Shanghai Tech University, Shanghai 200031, China;State Key Laboratory of Bio-Organic and Natural Products Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China;

关键词: Tandem allylic substitution;    WingPhos;    Protecting-group-free;    Palladium catalysis;    Enantioselectivity;   

DOI  :  

来源: DOAJ

【 摘 要 】

A protecting-group-free enantioselective tandem allylic substitution of o-phenylenediamines and o-aminophenols is realized for the first time with a Pd-WingPhos catalyst, providing expedient access to a series of chiral vinyl-substituted heterocycles in excellent ee and yields under mild reaction conditions. The protocol is applied successfully to the synthesis of a cholesteryl ester transfer protein (CETP) inhibitor.

【 授权许可】

Unknown