Improved Yields for the Palladium-Mediated 11C-Carbonylation Reaction Using Microwave Technology

• Published in: European journal of organic chemistry Vol. 2014; no. 2; pp. 307 - 310
• Main Authors: Dahl, Kenneth, Schou, Magnus, Rahman, Obaidur, Halldin, Christer
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 01.01.2014; WILEY‐VCH Verlag; Wiley Subscription Services, Inc
• Subjects: Carb­onylation; Isotopic labeling; Medicinal chemistry; Microwave chemistry; Microwave heating; Radiochemistry; Radiopharmaceuticals
• ISSN: 1434-193X; 1099-0690
• DOI: 10.1002/ejoc.201300989

Microwave heating technology was applied for the palladium‐mediated 11C‐carbonylation of aryl halides and triflates at ambient pressure using xantphos as supporting ligand. Improved yields were observed for the 11C‐aminocarbonylation of electron‐deficient aryl halides in comparison to thermal heating and the approach even allowed the use of an aryl chloride as substrate. The scope of this reaction was further extended to 11C‐labeled aryl acid and two 11C‐labeled aryl esters. Microwave heating was applied for the palladium‐mediated 11C‐carbonylation of aryl halides and triflates using xantphos as supporting ligand. Improved yields were observed for the 11C‐aminocarbonylation of electron‐deficient aryl halides in comparison to thermal heating and even allowed the use of an aryl chloride as substrate. A 11C‐labeled aryl acid and two 11C‐labeled aryl esters were also obtained.