Abstract
A method is described for the preparation of [ 11C]buprenorphine in high specific activity, based on the reaction of N-(de-cyclopropylmethyl)buprenorphine with “no carrier added” [1- 11C]cyclopropanecarbonyl chloride followed by reduction with lithium aluminium hydride. The [1- 11C]cyclo-propanecarbonyl chloride is itself prepared from cyclotron-produced [ 11C]carbon dioxide. The overall preparation time is 57 min from the end of radionuclide production, and the radiochemical yield is ca 20%, (decay-corrected from [ 11C]-carbon dioxide). [ 11C]Buprenophine has potential as a radio-ligand for the study of the opiate receptor system in vivo by means of position emission tomography.
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