Radiosynthesis of carbon-11 labeled 6-methyldopamine ([¹¹C]MeDA)

E Al-Momani; B D Zlatopolskiy; H-J Machulla; S N Reske; C Solbach

doi:10.1016/j.apradiso.2012.04.021

Radiosynthesis of carbon-11 labeled 6-methyldopamine ([¹¹C]MeDA)

Appl Radiat Isot. 2012 Aug;70(8):1475-9. doi: 10.1016/j.apradiso.2012.04.021. Epub 2012 May 1.

Authors

E Al-Momani¹, B D Zlatopolskiy, H-J Machulla, S N Reske, C Solbach

Affiliation

¹ Clinic for Nuclear Medicine, University Ulm, Germany.

PMID: 22728836
DOI: 10.1016/j.apradiso.2012.04.021

Abstract

A rapid and efficient n.c.a. radiosynthesis of 6-[(11)C]methyldopamine ([(11)C]MeDA) using the Stille cross-coupling reaction as a key step was developed. The labeling conditions for the formation of the intermediate compound (protected [(11)C]MeDA, [(11)C]7) were determined with respect to reaction temperature and time. The radiochemical yield 89 ± 1.4% (decay-corrected) of the protected intermediate [(11)C]7 was obtained at a reaction temperature of 60°C and a reaction time of 5 min using Pd(2)(dba)(3)/P(o-tolyl)(3) and CsF/CuBr as a co-catalyst system. The overall yield after deprotection with 45% HBr at 140°C for 10 min was 64 ± 3.9% (decay-corrected) within a total preparation time of 40 min, including hydrolysis, HPLC purification and formulation.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Carbon Radioisotopes / chemistry*
Deoxyepinephrine / chemical synthesis*
Hot Temperature

Substances

Carbon Radioisotopes
Deoxyepinephrine