摘要
Abstract
To synthesize [18 F]Florbetapir ,18 F-SPy5 ,18 F-SPm2 and 18 F-SPm5 ,18 F was labeled by nucleophilic substitution taking p-tosyloxy (OTs) as a leaving group to radio-synthesis [18F]Florbetapir for represent .The influences of precursor concentration , temperature and time on labeling reaction were investigated .The optimum conditions were established and taken as the labeling conditions for other 18 F labelled styryl nitrog-enous heterocycles .Then ,[18 F]Florbetapir ,18 F-SPy5 ,18 F-SPm2 ,and 18 F-SPm5 were synthesized by de-protecting t-Butyloxycarboryl (Boc) .The products were all separated by C18 cartridge and purified by semipreparative HPLC .Furthermore ,some necessary quality inspections were conducted on the pharmaceuticals so as to investigate the parameters ,such as basic physical and chemical characters , radiochemical , chemical purities and specific activity .The results showed that the optimum conditions for 18 F labeling were as follows :precursor concentration 1 g/L ,temperature 120 ℃ and time 10 minutes .The injections of [18 F]Florbetapir ,18 F-SPy5 ,18 F-SPm2 and 18 F-SPm5 were obtained ,which were all colorless and clear .For the injections ,the pH values were all 7-8 ,the radiochemical purities were all greater than 99％ ,the chemical purities were all higher than 98％ , and the specific activities were 1.09 × 107-5.11 × 107 MBq/g . It showed that nucleophilic substitution was an effective method for 18 F labeling .Under the selected conditions , the radiosynthesis progresses were stable and reliable , and injections of [18 F]Florbetapir ,18 F-SPy5 ,18 F-SPm2 and 18 F-SPm5 were obtained .The quality of the injections could satisfy experiment requirements .关键词
阿尔兹海默病(AD)/正电子发射断层显像(PET)/β淀粉样蛋白(Aβ)/18F/苯乙烯基氮杂环化合物Key words
Alzheimer's disease (AD)/positron emission tomography (PET )/β-Amy-loid (Aβ)/18 F/styryl nitrogenous heterocycles分类
能源科技
