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

Autor: E, Al-Momani, B D, Zlatopolskiy, H-J, Machulla, S N, Reske, C, Solbach
Rok vydání: 2012
Předmět:
Zdroj: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine. 70(8)
ISSN: 1872-9800
Popis: 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.
Databáze: OpenAIRE