Molecules, Vol. 24, Pages 4210: Late-Stage Copper-Catalyzed Radiofluorination of an Arylboronic Ester Derivative of Atorvastatin
Molecules, Vol. 24, Pages 4210: Late-Stage Copper-Catalyzed Radiofluorination of an Arylboronic Ester Derivative of Atorvastatin
Molecules doi: 10.3390/molecules24234210
Authors:
Gonçalo S. Clemente
Tryfon Zarganes-Tzitzikas
Alexander Dömling
Philip H. Elsinga
There is an unmet need for late-stage 18F-fluorination strategies to label molecules with a wide range of relevant functionalities to medicinal chemistry, in particular (hetero)arenes, aiming to obtain unique in vivo information on the pharmacokinetics/pharmacodynamics (PK/PD) using positron emission tomography (PET). In the last few years, Cu-mediated oxidative radiofluorination of arylboronic esters/acids arose and has been successful in small molecules containing relatively simple (hetero)aromatic groups. However, this technique is sparsely used in the radiosynthesis of clinically significant molecules containing more complex backbones with several aromatic motifs. In this work, we add a new entry to this very limited database by presenting our recent results on the 18F-fluorination of an arylboronic ester derivative of atorvastatin. The moderate average conversion of [18F]F− (12%), in line with what has been reported for similarly complex molecules, stressed an overview through the literature to understand the radiolabeling variables and limitations preventing consistently higher yields. Nevertheless, the current disparity of procedures reported still hampers a consensual and conclusive...
Source: Molecules - Category: Chemistry Authors: Gon çalo S. Clemente Tryfon Zarganes-Tzitzikas Alexander D ömling Philip H. Elsinga Tags: Communication Source Type: research
More News: Atorvastatin Calcium | Chemistry | Copper | Databases & Libraries | Lipitor | PET Scan | Statin Therapy | Zivast