Method for the use of [11c] carbon monoxide in labeling synthesis of 11c-labelled esters by photo-induced free radical carbonylation

Abstract

Methods and reagents for photo-initiated carbonylation with carbon-isotope labeled carbon monoxide using alkyl/aryl iodides with alcohols pretreated by a base are provided. The resultant carbon-isotope labeled esters are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.

1 .- 12 . (canceled) 
   
   
       13 . A carbon-isotope labeled compound of formula (III), 
     
       
         
         
             
             
         
       
     
     wherein R is linear or cyclic alkyl or substituted alkyl, aryl or substituted aryl 
   
   
       14 . A carbon-isotope labeled compound of  claim 13 , wherein R may contain chloro, fluoro, ester, carboxyl groups, which is separated by at least one carbon bearing the iodide atom. 
   
   
       15 . A kit for PET study comprising a carbon-isotope labeled compound of formula (III), 
     
       
         
         
             
             
         
       
     
     wherein R is linear or cyclic alkyl or substituted alkyl, aryl or substituted aryl 
   
   
       16 . A kit of  claim 15 , further comprising radioprotectant, antimicrobial preservative, pH-adjusting agent or filler. 
   
   
       17 . A kit of  claim 16 , wherein the radiopretectant is selected from ascorbic acid, para-aminobenzoic acid, gentisic acid and salts thereof. 
   
   
       18 . A kit of  claim 16 , wherein the antimicrobial preservative is selected from the parabens, benzyl alcohol, phenol, cresol, cetrimide and thiomersal. 
   
   
       19 . A kit of  claim 16 , wherein the pH-adjusting agent is a pharmaceutically acceptable buffer or a pharmaceutically acceptable base, or mixtures thereof. 
   
   
       20 . A kit of  claim 16 , wherein the filler is inorganic salts, water soluble sugars or sugar alcohols.