细胞凋亡显像剂~(18)F-ML-10前体合成及放射性标记

~(18)F-2-(5-氟-戊基)-2-甲基丙二酸(~(18)F-ML-10)是一个有潜力的细胞凋亡显像剂。以5-溴-1-戊醇为原料,合成了前体:5-甲基磺酰基戊基-2-甲基丙二酸二乙酯,采用国产MF-2V-IT-1模块,经亲核取代及碱水解,合成了~(18)F-ML-10;粗产品经HPLC纯化及固相萃取,得到~(18)F-ML-10注射液。18 F-ML-10的合成效率为(25.3±4.7)%(n=16,不校正),产品的放射化学纯度大于99%,比活度为740PBq/mol,K2.2.2含量低于10mg/L,有机溶剂乙腈残留量为(0.015±0.01)%(质量分数),无菌、无热原符合要求,产品满足临床研究需求。

Synthesis Precursor of Apoptosis Imaging Agent 18 F-ML-10 and Its Radiolabing With 18 F

18 F‐2‐(5‐fluoro‐pentyl)‐2‐methyl malonic acid(18 F‐M L‐10) is one of the competitive candidate for apoptosis imaging with PET .ML‐10 as reference and its OTs derivative (dieth‐yl 2‐methyl‐2‐(5‐(tosyloxy)pentyl) malonate) as precursor for labeling with fluorine‐18 were prepared .18 F‐ML‐10 was synthesized via nucleophilic substitution and base hydrolysis .The 18 F‐ML‐10 injection was got by semi‐HPLC and solid‐extraction‐preparation via home MF‐2V‐IT‐1 module .The synthesis yield of 18 F‐ML‐10 is (25.3 ± 4.7)% (n= 16 ,no corrected decay ) ,and the specific activity is 740 PBq/mol .T he radiochemical purity is over 99% .T he residuary acetonitrile in the injection is (0.015 ± 0.01)% (w) .The K2.2.2 mass concentra‐tion in the injection is low than 10 mg/L .The injection is free of bacteria and pyrogen .It can be used for clinical research .