A simple one-pot synthesis of cyclopropane [11C]carbonyl chloride. Synthesis and biodistribution of [11C]cyclorphan

✍ Scribed by Daniel W. McPherson; Dah-Ren Hwang; Joanna S. Fowler; Alfred P. Wolf; Robert M. Macgregor; Carroll D. Arnett

• Publisher: John Wiley and Sons
• Year: 1986
• Tongue: French
• Weight: 353 KB
• Volume: 23
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.2580230507

✦ Synopsis

N a t i o n a l Laboratory, Upton, NY 11973 Received Sumary A r a p i d , one-pot, s y n t h e s i s of cyclopropane [ llC]carbonyl c h l o r i d e was developed. This s y n t h e s i s proceeded i n 807; r a d i ochemical y i e l d (EOB) i n a s y n t h e s i s time of LO minutes. This a c i d c h l o r i d e was then used t o s y n t h e s i z e a model compound, [llC]cyclorphan, by a l k y l a t i o n of norlevorphanol followed by r e d u c t i o n of t h e i n t e r m e d i a t e [ llC]amide in an o v e r a l l s y n t h e s i s t i m e of 55 minutes and a radiochemical y i e l d of 15% (EOB).

The b i o d i s t r i b u t i o n of [ llC]cyclorphan in c o n t r o l and naloxone p r e t r e a t e d mice showed non-specific b i n d i n g and r a p i d c l e a r a n c e from b r a i n .