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报道了N 去甲基 Tamoxifen(N Demethyltamoxifen)和 11C标记Tamoxifen( 11C Tamox ifen)的制备及高效液相色谱 (HPLC)分离分析方法 .先将Tamoxifen柠檬酸盐 (TamoxifenCit rate)转换成无盐Tamoxifen(Tamoxifenfreebase) ,然后与 1 氯乙基 氯甲酸酯 (ACE Cl)反应生成N 去甲基 Tamoxifen .N 去甲基 Tamoxifen与 11CH3I在 1 3 0℃下反应 1 0min ,即生成 11C Tamoxifen .标记物用 μBonapakTMC18柱HPLC进行分离纯化后 ,制成 11C Tamoxifen注射液 .从停止核反应开始 ,整个标记及分离纯化过程需时 50～ 60min ,标记率可达 60 % .
Reported the preparation of N-demethylated Tamoxifen (N Demethyltamoxifen) and the 11C Tamoxifen (11C Tamoxifen), and high performance liquid chromatography (HPLC) separation and analysis methods. Tamoxifen citrate was first converted to salt-free Tamoxifen ( Tamoxifenfreebase), and then reacted with 1 chloroethyl chloroformate (ACE Cl) to form N-demethyl Tamoxifen.N desmethyl Tamoxifen reacted with 11CH3I at 130 ℃ for 10 min to generate 11C Tamoxifen. μBonapakTMC18 column HPLC separation and purification, made of 11C Tamoxifen injection.From stop nuclear reaction, the entire labeling and isolation and purification process takes 50 ~ 60min, labeling rate of up to 60%.