914299-59-5Relevant academic research and scientific papers
The Titanium-Mediated Double Reductive Cleavage of Cyclic Sulfonamides for the Synthesis of Aryl Pyrrolidines
Khalifa, Aisha,Evans, Paul
, p. 2969 - 2975 (2019/02/26)
Reduction of a range of benzo-fused cyclic sulfonamides has been accomplished using low-valent titanium. This operationally simple method generates the corresponding aryl-substituted cyclic amines, typically, with good conversion. Notably, unlike our previous Li-NH3-based method, loss of heteroatom-based substituents (X) on the aromatic ring does not readily occur, and the robustness of this method was demonstrated with a synthesis of the Sceletium alkaloid mesembrane.
Synthesis of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1,2,4-triazines that have antibacterial activity and also inhibit inorganic pyrophosphatase
Lv, Wei,Banerjee, Biplab,Molland, Katrina L.,Seleem, Mohamed N.,Ghafoor, Adil,Hamed, Maha I.,Wan, Baojie,Franzblau, Scott G.,Mesecar, Andrew D.,Cushman, Mark
, p. 406 - 418 (2014/01/17)
Inorganic pyrophosphatases are potential targets for the development of novel antibacterial agents. A pyrophosphatase-coupled high-throughput screening assay intended to detect o-succinyl benzoic acid coenzyme A (OSB CoA) synthetase inhibitors led to the unexpected discovery of a new series of novel inorganic pyrophosphatase inhibitors. Lead optimization studies resulted in a series of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1,2,4-triazine derivatives that were prepared by an efficient synthetic pathway. One of the tetracyclic triazine analogues 22h displayed promising antibiotic activity against a wide variety of drug-resistant Staphylococcus aureus strains, as well as activity versus Mycobacterium tuberculosis and Bacillus anthracis, at a concentration that was not cytotoxic to mammalian cells.
