Füchtner F, Angelberger P, Kvaternik H, Hammerschmidt F, Simovc B Peric, Steinbach J
Institute of Bioorganic and Radiopharmaceutical Chemistry, Forschungszentrum Rossendorf, D-01314, Germany.
Nucl Med Biol. 2002 May;29(4):477-81. doi: 10.1016/s0969-8051(02)00298-6.
A modified method for the synthesis of the intermediate product N-Boc-3,4-di(Boc-O)-6-iodo-L-phenylalanine ethyl ester of the [18F]FDOPA precursor preparation was developed. With the application of bis-(trifluoroacetoxy)-iodobenzene for the iodination step with elemental iodine the yield of the intermediate can be increased from 12% to 50-60%. By replacing silica-gel-based RP HPLC column by a polymer-based column for semi-preparative purification of [18F]FDOPA from the reaction mixture the radiochemical purity of the final product can be increased up to >99%. For the determination of the radiochemical impurity [18F]fluoride a HPLC method using a column with polymer-based RP material was introduced.
开发了一种改进的方法用于合成[¹⁸F]FDOPA前体制剂的中间体N-Boc-3,4-二（Boc-O）-6-碘-L-苯丙氨酸乙酯。在碘化步骤中使用双（三氟乙酰氧基）碘苯代替单质碘，中间体的产率可从12%提高到50-60%。通过用聚合物基柱代替硅胶基RP HPLC柱从反应混合物中对[¹⁸F]FDOPA进行半制备纯化，最终产品的放射化学纯度可提高至>99%。为了测定放射化学杂质[¹⁸F]氟化物，引入了一种使用基于聚合物的RP材料柱的HPLC方法。
