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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Studies Directed Towards The Iridium Catalyzed Synthesis Of New Carbon-Nitrogen Bonds., Maria Lindsay May 2017

Studies Directed Towards The Iridium Catalyzed Synthesis Of New Carbon-Nitrogen Bonds., Maria Lindsay

University of New Orleans Theses and Dissertations

Amines are ubiquitous in nature and serve a variety of functions in living organisms. Because of this fact amines are of great biological and pharmaceutical interest. The iridium catalyst (pentamethylcyclopentadienyl) iridium dichloride dimer ([Cp*IrCl2]2) has been used in a number of ways to synthesize new carbon-nitrogen bonds. These studies were directed toward the development of a method for the iridium catalyzed N-alkylation of alpha-amino acid esters as well as the development of a strategy for synthesis of the natural product 275A.

We have optimized a method for the N-alkylation for alpha-amino acid esters. Using this …


Copper Salt-Catalyzed Formation Of A Novel Series Of Triazole-Spirodienone Conjugates With Potent Anticancer Activity., L. Gu, P. Wang, Qiu Zhong, Y. Deng, J. Xie, F. Liu, F. Xiao, Shilong Zheng, Y. Chen, Guangdi Wang, L. He Jan 2017

Copper Salt-Catalyzed Formation Of A Novel Series Of Triazole-Spirodienone Conjugates With Potent Anticancer Activity., L. Gu, P. Wang, Qiu Zhong, Y. Deng, J. Xie, F. Liu, F. Xiao, Shilong Zheng, Y. Chen, Guangdi Wang, L. He

Faculty and Staff Publications

Copper salt-catalyzed oxidative amination resulted in the formation of a novel series of triazole-spirodienone conjugates, 4-triazolyl-1-oxa-4-azaspiro[4,5]deca-6,9-dien-3,8-diones and 4-triazolyl-1-oxa-4-azaspiro[4,5]deca-6,9-dien-8-ones. A single crystal of compound 1p among them was grown and analyzed by X-ray crystallography. These compounds were evaluated for their antiproliferative activities against MDA-MB-231, HeLa, A549 and MCF-7 cell lines. Most of them showed moderate to high anticancer potency in the four cancer cell lines. The discovery of the triazole-spirodienone conjugates as cytotoxic agents against cancer cells may open up a new field in which these novel small molecules could be further explored as promising anticancer agents.