A facile and rapid automated synthesis of 3'-deoxy-3'-[(18)F]fluorothymidine.
OBJECTIVE
To develop a simplified and fully automated synthesis procedure of 3'-deoxy-3'-[(18)F]fluorothymidine ([(18)F]FLT) using PET-MF-2V-IT-I synthesis module.


METHODS
Synthesis of [(18)F]FLT was performed using PET-MF-2V-IT-I synthesis module by one-pot two-step reaction procedure, including nucleophilic fluorination of 3-N-t-butoxycarbonyl-1-[5'-O-(4,4'-dimethoxy triphenylmethyl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl)-beta-d-threopentofuranosyl]thymine (15mg) as the precursor molecule with [(18)F]fluoride, and subsequent hydrolysis of the protecting group with 1.0M HCl at the same reaction vessel and purification with SEP PAK cartridges instead of the HPLC system.


RESULTS
The automated synthesis of [(18)F]FLT with SEP PAK purification gave corrected radiochemical yield of 23.2+/-2.6% (n=6, uncorrected yield: 16-22%) and radiochemical purity of >97% within the total synthesis time of 35min.


CONCLUSIONS
The fully one-pot automated synthesis procedure with SEP PAK purification can be applied to the fully automated synthesis of [(18)F]FLT using commercial [(18)F]FDG synthesis module.
Tang
Ganghua
G
PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China. gtang0224@yahoo.com.cn
Tang
Xiaolan
X
Wen
Fuhua
F
Wang
Mingfang
M
Li
Baoyuan
B
D015224:Dideoxynucleosides / Q000737:chemistry* / Q000302:isolation & purification*; D007553:Isotope Labeling / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000302:isolation & purification*; D012371:Robotics / Q000379:methods*
D015224:Dideoxynucleosides; D019275:Radiopharmaceuticals; C002854:alovudine