Periodic Reporting for period 1 - COOPCAT (Cooperative Lewis base / Metal-Catalyzed Enantioselective Annulations)
Okres sprawozdawczy: 2019-06-01 do 2021-05-31
Five to seven-membered heterocycles are of immense use biologically and industrially. Heterocycles are present in all types of organic compounds of interest in electronics, optics, biology, pharmacology, material sciences, etc. Five to seven-membered heterocycles impart an important function in medicinal chemistry and serve as key templates for the development of many therapeutic agents. There are many common therapeutic uses of synthetic heterocycles such as antibacterial, trypanocidal, antimycobacterial, genotoxic, anti-HIV activity, herbicidal, anti-inflammatory, analgesic, antileishmanial agents, muscle relaxants, anticonvulsant, anticancer, antifungal antimalarial, antitubercular, hypnotics, anthelmintic, antidepressant, antitumoral, and insecticidal agents. The exploration of new bioactive heterocyclic analogs continues to be an area of intensive research in pharmaceutical chemistry. The project set out to devise new efficient ways to make such molecules.
The initial approach to the target molecules turned out to be unsuccessful, but an alternative method based on organolithium photochemistry did deliver useful products, and two publications are in the process of being edited ready for dissemination.
The alternative methods developed have shown that mild photochemical methods using LED irradiation can push forward the state of the art in synthetic photochemistry - this was not part of the original proposal, that was discovered while attempting to solve the problems that were encountered during the project. This aspect of the work has a significant future potential impact in synthesis as it will allow low energy bulbs to be used for heterocyclic synthesis in routes that employ reactive intermediates as chromophores.
Further project proposals will be developed in which such a reaction is employed as a key step.
Further project proposals will be developed in which such a reaction is employed as a key step.