Automated radiochemical synthesis of pharmaceutical grade [(18) F]FLT using 3-N-Boc-5'-O-dimethoxytrityl-3'-O-nosyl-thymidine precursor and its Sep-Pak® purification employing selective elution from reversed phase.

Pharmaceutical grade 3'-deoxy-3'-[18 F]fluorothymidine [18 F]FLT was synthesized using 3-N-Boc-5'-O-dimethoxytrityl-3'-O-nosyl-thymidine (BOC-Nosyl) precursor, in the general purpose TRACERlab FX modules. Purification of [18 F]FLT, via solid phase extraction (SPE) after radiosynthesis, using a combination of different SPE cartridges, yielded satisfactory results, with radiochemical and chemical purity >99%. While the non-decay corrected radiochemical yield (RCY) with 20 mg (24 μmole) of BOC-Nosyl precursor was found to be 6.80 ± 0.16%, the decay corrected radiochemical yield (RCY) was 9.95 ± 0.24%. Residual acetone, acetonitrile, and ethanol levels were found to be 22.97 ± 0.76, 109.08 ± 0.93, and 7,666.45 ± 3.7 ppm, respectively. A simplified method for solid-phase purification of [18 F]FLT was developed, circumventing the need for HPLC purification. Biodistribution in C57BL/6 mice with B16F10 cell line-induced melanoma showed tumor to blood ratio of ~3.8 at 90 min. PET/CT imaging of normal rabbit injected with [18 F]FLT shows selective uptake in the bone marrow and small intestine. [18 F]FLT was found to be excreted through the kidneys and get collected in the urinary bladder, 120 min post injection. PET/CT imaging performed in rabbit model at 30, 60, 90, and 120 min post [18 F]FLT injections showed concordance with tissue distribution kinetics of mice tumor model.

Mitra A ，Chakraborty A ，Upadhye T ，Tawate M ，Lad S ，Sahu S ，Rajesh C ，Bagul S ，Pawar Y ，Ray MK ，Banerjee S ... -  《-》

Automated Optimized Synthesis of [(18)F]FLT Using Non-Basic Phase-Transfer Catalyst with Reduced Precursor Amount.

Fedorova OS ，Orlovskaya VV ，Krasikova RN 《MOLECULES》

Efficient radiosynthesis of 3'-deoxy-3'-18F-fluorothymidine using electrowetting-on-dielectric digital microfluidic chip.

Javed MR ，Chen S ，Kim HK ，Wei L ，Czernin J ，Kim CJ ，van Dam RM ，Keng PY ... -  《-》

High radiochemical yield synthesis of 3'-deoxy-3'-[18F]fluorothymidine using (5'-O-dimethoxytrityl-2'-deoxy-3'-O-nosyl-beta-D-threo pentofuranosyl)thymine and its 3-N-BOC-protected analogue as a labeling precursor.

Yun M ，Oh SJ ，Ha HJ ，Ryu JS ，Moon DH ... -  《NUCLEAR MEDICINE AND BIOLOGY》

[Quality Control and Biological Assessment of Automated Synthesized 3'-deoxy-3'-¹⁸F-fluorothymidine using CFN-MPS-200 Module].

Jiang X ，Wang XX ，Lu H ，Chen SR ，Xiao DQ ，Zhao M ，Li XL ，Zhang G ，Xu GH ，Cheng ZZ ... -  《-》