An Improved Synthesis of PET Dopamine D2 Receptors Radioligand [11C]Raclopride
Authors:
- 31 December 2004
- journal article
- Published by Taylor & Francis in Synthetic Communications
- Vol. 34 (10) , 1897-1907
Abstract
An improved synthesis of [11C]raclopride is reported. The precursor desmethyl‐raclopride was synthesized from 3,5‐dichloro‐2,6‐dimethoxybenzoic acid and (S)‐(−)‐2‐aminoethyl‐1‐ethylpyrrolidine via a straightforward, four‐step synthetic approach with 29% overall chemical yield. [11C]Raclopride was prepared by O‐[11C]methylation of the precursor with [11C]methyl triflate and purification with a semi‐preparative HPLC method in 20–34% radiochemical yield, based on [11C]methyl bromide, decay corrected to end of bombardment (EOB).Keywords
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