Efficient 11C-carbonylation of isolated aryl palladium complexes for PET: application to challenging radiopharmaceutical synthesis.
J Am Chem Soc
; 137(4): 1548-55, 2015 Feb 04.
Article
in En
| MEDLINE
| ID: mdl-25569730
ABSTRACT
We describe the successful implementation of palladium-aryl oxidative addition complexes as stoichiometric reagents in carbonylation reactions with (11)CO to produce structurally challenging, pharmaceutically relevant compounds. This method enables the first (11)C-carbonyl labeling of an approved PET tracer, [(11)C]raclopride, for the dopamine D2/D3 receptor by carbonylation with excellent radiochemical purity and yield. Two other molecules, [(11)C]olaparib and [(11)C]JNJ 31020028, were efficiently labeled in this manner. The technique distinguishes itself from existing methods by the markedly improved purity profiles of the tracer molecules produced and provides access to complex structures in synthetically useful yields, hereby offering a viable alternative to other (11)C-labeling strategies.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Palladium
/
Carbon Radioisotopes
/
Radiopharmaceuticals
/
Coordination Complexes
Language:
En
Journal:
J Am Chem Soc
Year:
2015
Type:
Article
Affiliation country:
Denmark