Electrophilic aromatic substitution of azines catalysed by Frustrated Lewis pairs

Informations projet

LEWIS-PYR

N° de convention de subvention: 894998

DOI

10.3030/894998

Projet clôturé

Date de signature de la CE 24 Mars 2020

Date de début 1 Mai 2021

Date de fin 30 Avril 2023

Financé au titre de

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Coût total

€ 172 932,48

Contribution de l’UE

€ 172 932,48

Coordonné par

FUNDACIO INSTITUT CATALA D'INVESTIGACIO QUIMICA
Spain

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

Période du rapport: 2021-05-01 au 2023-04-30

Résumé du contexte et des objectifs généraux du projet

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.

Travail effectué depuis le début du projet jusqu’à la fin de la période considérée dans le rapport et principaux résultats atteints jusqu’à présent

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.

Progrès au-delà de l’état des connaissances et impact potentiel prévu (y compris l’impact socio-économique et les conséquences sociétales plus larges du projet jusqu’à présent)

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