Preparation of [11C]buprenorphine—A potential radioligand for the study of the opiate receptor system in vivo

✍ Scribed by Sajinder K. Luthra; Victor W. Pike; Frank Brady; Peter L. Horlock; Christian Prenant; Christian Crouzel

• Book ID: 103920000
• Publisher: Elsevier Science
• Year: 1987
• Weight: 185 KB
• Volume: 38
• Category: Article
• ISSN: 0883-2889
• DOI: 10.1016/0883-2889(87)90239-5

✦ Synopsis

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.