Project 12

Development of late-stage and rapid carboxylation techniques with ¹⁴CO₂ in drug development programs (WP4)

Host institution: AstraZeneca AB, Sweden
Application Deadline: 22nd February
3 PhD year position. Expected start date: Mid 2020.
Remember to read the eligibility criteria here.

Objectives:

1. Investigate the application of alkyl halides and pseudohalides for the synthesis of alkyl–Ni complexes and their ability to undergo rapid carboxylations with ¹⁴CO₂ in the presence of a reductant
2. Adapt new electrochemical and photolytic methods for the transformation of alkyl silicates to corresponding carboxylates with ¹⁴CO₂ applying Ni-complexes
3. Apply the developed conditions for late stage ¹⁴C labelling of pharmaceutically relevant alkyl carboxylates

Expected results:

1. New techniques for late-stage carbon-14 isotope labelling adaptable to drug development programs
2. A detailed understanding of the steps involved in transition metal-mediated carboxylations, particularly with nickel.
3. Fast carboxylation reactions with easy-to-prepare intermediates

Planned secondment(s):

ESR12 has its daily work at the industrial site AZ, and will therefore have two academic secondments.

• AU to Prof. Skrydstrup (3 months): Development of electrochemical methods for the rapid carboxylation of alkyl silicates (with ESR9).
• ICIQ to Prof. Martin (3 months): Analysis of individual steps in the carboxylation of alkyl-Ni intermediates (with ESR1).

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Enrolment in Doctoral degree(s): ESR12 will have the daily work at AstraZeneca, Sweden, but will be formally enrolled at Aarhus University, Denmark

Principal Supervisor: Prof. Charles Elmore (AZ)

Questions? Write to us at co2perate@uit.no.