A direct fixation of CO2 for isotopic labelling of hydantoins using iodine–phosphine charge transfer complexes. Issue 54 (15th June 2022)

• Record Type: Journal Article
• Authors: Bow, John-Paul J.; Adami, Valentina; Marasco, Agostino; Grønnevik, Gaute; Rivers, Dean A.; Alvaro, Guiseppe; Riss, Patrick J.
• Is Part Of: Chemical communications. Volume 58:Issue 54(2022)
• Page Start: 7546
• Page End: 7549
• Publication Date: 2022-06-15
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d2cc01754g
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Herein, we report a method for the isotopic labelling of hydantoins directly from CO2 by means of trimethyl-λ 5 -phosphine diiodide mediated carbonyl insertion. Abstract : Herein, we report a method for the isotopic labelling of hydantoins directly from CO2 by means of trimethyl-λ 5 -phosphine diiodide mediated carbonyl insertion. The method is suitable for 13 C-labelling of diverse substrates and was implementated for 11 C-labelling in PET-imaging facilities for the synthesis of radiotracers. Isolated yields of 90% and radiochemical yields of 89% were achieved for hydantoin containing drug candidates in formulation within 30 min with high molar activity (>400 MBq nmol −1 ).