Electrophilic aromatic substitution of azines catalysed by Frustrated Lewis pairs

Project Information

LEWIS-PYR

Grant agreement ID: 894998

DOI

10.3030/894998

Project closed

EC signature date 24 March 2020

Start date 1 May 2021

End date 30 April 2023

Funded under

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Total cost

€ 172 932,48

EU contribution

€ 172 932,48

Coordinated by

FUNDACIO INSTITUT CATALA D'INVESTIGACIO QUIMICA
Spain

Periodic Reporting for period 1 - LEWIS-PYR (Electrophilic aromatic substitution of azines catalysed by Frustrated Lewis pairs)

Reporting period: 2021-05-01 to 2023-04-30

Summary of the context and overall objectives of the project

Pyridine is the most common nitrogen-containing aromatic heterocycle employed as the core structure in a number of drugs in the pharmaceutical science. Since the discovery of first deuterated drug, these compounds are crucial for applicability in absorption, distribution, metabolism, and excretion (ADME) studies, and indicated vital roles in medicinal chemistry via boosting pharmacokinetic and pharmacodynamic properties of drug. Therefore, it is very much important to provide site-selective methodology for installation of hydrogen isotopes at various positions of pyridine and related heterocycles. Our research laboratory found that a range of pyridine containing heterocycles can be labeled with deuterium in site-selective manner. This discovery will open door for new types of deuterium labelled pharmaceutical drugs.

Work performed from the beginning of the project to the end of the period covered by the report and main results achieved so far

We have provide very useful technology for site-selective deuterium labelling in pyridine containing heterocycles such as pyrazolo[1,5-a]pyridine and [1,2,3]triazolo[1,5-a]pyridine. Site-selectivity was controlled by right combination of base and deuterium source.
A draft of the key results from this project is being prepared to focus on the base-mediated site-selective deuterium labelling of pyridine containing heterocycles. This work will be submitted to an internationally leading journal and made available as open access (OA). This will be further advertised via the host group webpage.

Progress beyond the state of the art and expected potential impact (including the socio-economic impact and the wider societal implications of the project so far)

In the last one year, SCG has applied for few scientist positions such as Assistant Professor in the IITs (Indian Institutes of Technology) and BITS Pilani (Birla Institute of Technology and Science) and these processes are ongoing with SCG waiting for an interview call. In the meantime, the researcher has secured a research scientist position in Research and Development (R&D) department in one of the top fine and specialty chemical manufacturing company located in India (Clean Science and Technology Limited). In the new position, he will mainly work on developing ingenious technologies with unique, innovative, sustainable and cost effective catalytic manufacturing processes

LEWIS-PYR: De novo catalytic route for enabling SEAr of azines