Luthra S K, Pike V W, Brady F, Horlock P L, Prenant C, Crouzel C
Int J Rad Appl Instrum A. 1987;38(1):65-6. doi: 10.1016/0883-2889(87)90239-5.
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]cyclopropanecarbonyl 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]Buprenorphine has potential as a radioligand for the study of the opiate receptor system in vivo by means of position emission tomography.
