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LABEL-DIOX

Late-stage catalytic carboxylation techniques with labelled carbon dioxide: new opportunities for radiolabelling

Total Cost €

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EC-Contrib. €

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Partnership

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Project "LABEL-DIOX" data sheet

The following table provides information about the project.

Coordinator
FUNDACIO PRIVADA INSTITUT CATALA D'INVESTIGACIO QUIMICA 

Organization address
address: AVENIDA PAISSOS CATALANS 16
city: TARRAGONA
postcode: 43007
website: www.iciq.es

contact info
title: n.a.
name: n.a.
surname: n.a.
function: n.a.
email: n.a.
telephone: n.a.
fax: n.a.

 Coordinator Country Spain [ES]
 Total cost 149˙750 €
 EC max contribution 149˙750 € (100%)
 Programme 1. H2020-EU.1.1. (EXCELLENT SCIENCE - European Research Council (ERC))
 Code Call ERC-2016-PoC
 Funding Scheme ERC-POC
 Starting year 2017
 Duration (year-month-day) from 2017-12-01   to  2019-05-31

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    FUNDACIO PRIVADA INSTITUT CATALA D'INVESTIGACIO QUIMICA ES (TARRAGONA) coordinator 149˙750.00

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 Project objective

Absorption, distribution, metabolism and excretion´s studies (ADME) are essential for drug discovery and development, providing invaluable preclinical data to understand how the drug behaves in living organisms, thus allowing to make a decision on whether the drug should be terminated or advanced to the next step. At present, most of these studies are performed with a radiolabelled 14C-labelled version of the drug; unfortunately, current radiolabelling syntheses rely on lengthy-step sequences or rather expensive 14C-labelled building blocks, dramatically raising the costs for the research and development, and delaying the execution of preclinical studies. Taking into consideration that carboxylic acids are privileged motifs in a myriad of agrochemicals or pharmaceuticals, LABEL-DIOX offers the opportunity of promoting a late-stage carboxylation event with labeled CO2. The protocol is user-friendly, with components that are neither air- nor moisture sensitive, utilizes earth-abundant catalysts and operates under mild conditions. LABEL-DIOX will increase the overall efficiency of the carbon isotope incorporation, reduce the costs that would have resulted from the design of a lengthy radiolabelled synthesis, minimize the costs for waste disposal and dramatically increase the revenues, thus changing the way industrial chemists conduct radiolabelling of drugs containing carboxylic acids.

 Publications

year authors and title journal last update
List of publications.
2019 Andreu Tortajada, Yaya Duan, Basudev Sahoo, Fei Cong, Georgios Toupalas, Antoine Sallustrau, Olivier Loreau, Davide Audisio, Ruben Martin
Catalytic Decarboxylation/Carboxylation Platform for Accessing Isotopically Labeled Carboxylic Acids
published pages: 5897-5901, ISSN: 2155-5435, DOI: 10.1021/acscatal.9b01921
ACS Catalysis 9/7 2019-11-26

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