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 ...

Related Articles:

Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1, 6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties

[Zeng, Li-Fan; Wang, Yong; Kazemi, Roza; Xu, Shili; Xu, Zhong-Liang; Sanchez, Tino W.; Yang, Liu-Meng; Debnath, Bikash; Odde, Srinivas; Xie, Hua; Zheng, Yong-Tang; Ding, Jian; Neamati, Nouri; Long, Ya-Qiu Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9492 - 9509]

Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1, 6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties

[Zeng, Li-Fan; Wang, Yong; Kazemi, Roza; Xu, Shili; Xu, Zhong-Liang; Sanchez, Tino W.; Yang, Liu-Meng; Debnath, Bikash; Odde, Srinivas; Xie, Hua; Zheng, Yong-Tang; Ding, Jian; Neamati, Nouri; Long, Ya-Qiu Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9492 - 9509]

Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1, 6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties

[Zeng, Li-Fan; Wang, Yong; Kazemi, Roza; Xu, Shili; Xu, Zhong-Liang; Sanchez, Tino W.; Yang, Liu-Meng; Debnath, Bikash; Odde, Srinivas; Xie, Hua; Zheng, Yong-Tang; Ding, Jian; Neamati, Nouri; Long, Ya-Qiu Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9492 - 9509]

Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1, 6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties

[Zeng, Li-Fan; Wang, Yong; Kazemi, Roza; Xu, Shili; Xu, Zhong-Liang; Sanchez, Tino W.; Yang, Liu-Meng; Debnath, Bikash; Odde, Srinivas; Xie, Hua; Zheng, Yong-Tang; Ding, Jian; Neamati, Nouri; Long, Ya-Qiu Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9492 - 9509]

Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1, 6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties

[Zeng, Li-Fan; Wang, Yong; Kazemi, Roza; Xu, Shili; Xu, Zhong-Liang; Sanchez, Tino W.; Yang, Liu-Meng; Debnath, Bikash; Odde, Srinivas; Xie, Hua; Zheng, Yong-Tang; Ding, Jian; Neamati, Nouri; Long, Ya-Qiu Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9492 - 9509]

More Articles...