Preparation of ^(11)C labelled tamoxifen

The syntheses and HPLC analysis of N-desmethyltamoxifen and carbon11 labelled tamoxifen are described.In order to obtain the N-desmethyltamoxifen,tamoxifen citrate was first converted to tamoxifen free base.N-desmethyltamoxifen was prepared by reacting tamoxifen free base with 1-chloroethyl-chloroformate(ACE.C1). For ^11C labeling,N-desmethyltamoxifen was heated with ^11C methyl iodide for 10min at 130℃,and the 11C labelled compund was purified by HPLC on a μBonapak TM C18 column,Injectable ^11C-tamoxifen was obtained within 50-60 min from EOB (end-of -bombardment)with a labeling yield of 60%-70%.

The syntheses and HPLC analysis of N-desmethyltamoxifen and carbon-11 labelled tamoxifen are described. In order to obtain the N-desmethyltamoxifen, tamoxifen citrate was first converted to tamoxifen free base. N-desmethyltamoxifen was prepared by reacting tamoxifen free base with l-chloroethyl-chloroformate(ACE.CI). For11C labeling, N-desmethyltamoxifen was heated with11C methyl iodide for l0min at 130℃, and the 11C labelled compound was purified by HPLC on a μBonapak TM C18 column. Injectable 11C-tamoxifen was obtained within 50~60 min from EOB (end-of-bombardment) with a labeling yield of 60％~70％.