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

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.

Host institution

FUNDACIO PRIVADA INSTITUT CATALA D'INVESTIGACIO QUIMICA
Net EU contribution
€ 149 750,00
Address
Avenida Paissos Catalans 16
43007 Tarragona
Spain

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Region
Este Cataluña Tarragona
Activity type
Research Organisations
Non-EU contribution
€ 0,00

Beneficiaries (1)

FUNDACIO PRIVADA INSTITUT CATALA D'INVESTIGACIO QUIMICA
Spain
Net EU contribution
€ 149 750,00
Address
Avenida Paissos Catalans 16
43007 Tarragona

See on map

Region
Este Cataluña Tarragona
Activity type
Research Organisations
Non-EU contribution
€ 0,00