On-line [11C]methylation using [11C]methyl iodide for the automated preparation of 11C-radiopharmaceuticals.
A novel method for the efficient preparation of 11C-radiopharmaceuticals by on-line [11C]methylation using [11C]methyl iodide has been developed and applied to a rapid, convenient automated system. [11C]Methyl iodide is first trapped in a short column, containing an adsorber and coated substrate, which is connected to an HPLC injector. DMF is then introduced. Alternatively the substrate is added with the DMF. A whole reaction mixture can be easily injected onto an HPLC column for purification by switching the injector valve immediately after the reaction. Thus, radiochemical yields in the preparation of 11C-labeled doxepin, benztropine, cyproheptadine and N-methylspiperone have been improved remarkably and the synthetic procedure simplified.
Iwata
R
R
CYRIC Tohoku University, Sendai, Japan.
Pascali
C
C
Yuasa
M
M
Yanai
K
K
Takahashi
T
T
Ido
T
T
D001590:Benztropine; D002250:Carbon Radioisotopes; D003533:Cyproheptadine; D004316:Doxepin; D006847:Hydrocarbons, Iodinated; D007553:Isotope Labeling; D008745:Methylation; D013134:Spiperone / Q000031:analogs & derivatives
D002250:Carbon Radioisotopes; D006847:Hydrocarbons, Iodinated; D004316:Doxepin; D001590:Benztropine; D003533:Cyproheptadine; D013134:Spiperone; C039167:3-N-methylspiperone; C014055:methyl iodide