An Improved Synthesis of PET Dopamine D2 Receptors Radioligand [11C]Raclopride

Autor:	Xiangshu Fei, Qi Huang Zheng, Barbara E. Glick-Wilson, Michael L. Sullivan, Ji Quari Wang, Gary D. Hutchins, Bruce H. Mock, Timothy R. DeGrado
Rok vydání:	2004
Předmět:	Raclopride Chemistry Organic Chemistry Analytical chemistry Methylation Medicinal chemistry 11c raclopride chemistry.chemical_compound Bromide Yield (chemistry) Dopamine receptor D2 Radioligand medicine Receptor medicine.drug
Zdroj:	Synthetic Communications. 34:1897-1907
ISSN:	1532-2432 0039-7911
DOI:	10.1081/scc-120034174
Popis:	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).
Databáze:	OpenAIRE
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