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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-desmethyltamoxffen was prepared by reacting tamoxifen free base with 1-chloroethyl-chloroformate(ACE.Cl). For ~(11)C labeling, N-desmethyltamoxifen was heated with ~(11)C methyl iodide for 10min at 130℃, and the ~(11)C labelled compound was purified by HPLC on a μBonapak TM C_(18) column. Injectable ~(11)C-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 carbon11 labeled tamoxifen are described. In order to obtain the N-desmethyltamoxifen, tamoxifen citrate was first converted to tamoxifen free base. N-desmethyltamoxffen was prepared by reacting tamoxifen free base with 1-chloroethyl- (11) C labeling, N-desmethyltamoxifen was heated with ~ (11) C methyl iodide for 10 min at 130 ° C and the ~ (11) C labeled compound was purified by HPLC on a μBonapak TM C_ (18) column. Injectable ~ (11) C-tamoxifen was obtained within 50 ~ 60 min from EOB (end-of-bombardment) with a labeling yield of 60% ~ 70%.