Electrophilic aromatic substitution of azines catalysed by Frustrated Lewis pairs

Projektinformationen

LEWIS-PYR

ID Finanzhilfevereinbarung: 894998

DOI

10.3030/894998

Projekt abgeschlossen

EK-Unterschriftsdatum 24 März 2020

Startdatum 1 Mai 2021

Enddatum 30 April 2023

Finanziert unter

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Gesamtkosten

€ 172 932,48

EU-Beitrag

€ 172 932,48

Koordiniert durch

FUNDACIO INSTITUT CATALA D'INVESTIGACIO QUIMICA
Spain

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

Berichtszeitraum: 2021-05-01 bis 2023-04-30

Zusammenfassung vom Kontext und den Gesamtzielen des Projekts

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.

Arbeit, die ab Beginn des Projekts bis zum Ende des durch den Bericht erfassten Berichtszeitraums geleistet wurde, und die wichtigsten bis dahin erzielten Ergebnisse

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.

Fortschritte, die über den aktuellen Stand der Technik hinausgehen und voraussichtliche potenzielle Auswirkungen (einschließlich der bis dato erzielten sozioökonomischen Auswirkungen und weiter gefassten gesellschaftlichen Auswirkungen des Projekts)

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