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

Autor:	Sven N. Reske, Ehab Al-Momani, Christoph Solbach, Boris D. Zlatopolskiy, Hans-Juergen Machulla
Rok vydání:	2012
Předmět:	Methyldopamine chemistry.chemical_compound Radiation Chemistry Stereochemistry Yield (chemistry) Radiosynthesis Cardiovascular agent Solvolysis Chemical reaction Medicinal chemistry MEDA Stille reaction
Zdroj:	Applied Radiation and Isotopes. 70:1475-1479
ISSN:	0969-8043
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
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::2cf39bd1e63fb2098dd7a16c4db99e73 https://doi.org/10.1016/j.apradiso.2012.04.021 Zobrazit plný text záznamu Full Text from ScienceDirect