Copper-Catalyzed C–N Coupling in the Synthesis of Integrase Inhibitors of Immunodeficiency Viruses

…, IN Houpis, R Liu, Y Wang, J Zhang

Index: Lin, Jinguan; Houpis, Ioannis N.; Liu, Renmao; Wang, Youchu; Zhang, Jianqian Organic Process Research and Development, 2014 , vol. 18, # 1 p. 205 - 214

Full Text: HTML

Citation Number: 2

Abstract

This contribution describes the total synthesis of a complex macrocyclic integrase inhibitor, a key enzyme involved in the infection process of various immunodeficiency viruses. The key transformation of the synthetic strategy was the selective C–N coupling of a sulfonamide to a heteroaryl bromide in the presence of potentially competing amide and carbamate functionalities. The transformation was accomplished with CuI catalysis using bypiridine ...