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%.
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