A study of the radiosynthesis of fac-[¹⁸⁸ReCO₃(H₂O)₃]⁺ and its application in labeling 1,2,3-triazole analogs obtained by click chemistry.
OBJECTIVE
To optimize the conditions for the preparation of the organometallic precursor fac-[¹⁸⁸ReCO₃(H₂O)₃]⁺ and to synthesize the radiolabeling compounds of tricarbonyl rhenium. 1,2,3-Triazole analogs were synthesized by click chemistry and labeled with fac-[ReCO₃(H₂O)₃]Br and fac-[¹⁸⁸ReCO₃(H₂O)₃]⁺. The aim was to improve the methods for the synthesis of ¹⁸⁸Re-labeled radiopharmaceuticals for therapy.


METHODS
With potassium boranocarbonate as the CO source and ammonia borane as the reducing agent, fac-[¹⁸⁸ReCO₃(H₂O)₃]⁺ was synthesized, and the click chemistry method was used to prepare the tricarbonyl rhenium complex.


RESULTS
At the optimal reaction condition (the amounts of K₂[H₃BCO₂] and BH₃·NH₃ are 5 and 5 mg, respectively; reaction temperature is 75°C; and reaction time is 15 min), the radiochemical yields were 90%, and the labeling yield of bis(pyridin-2-ylmethyl) amine with fac-[¹⁸⁸ReCO₃(H₂O)₃]⁺ was more than 99% in 1 h at 75°C; the conjugation yields of triazole analog obtained by click chemistry with 'cold' and 'radio' tricarbonyl rhenium were more than 80%.


CONCLUSIONS
The organometallic precursor fac-[¹⁸⁸ReCO₃(H₂O)₃]⁺ was prepared under optimal reaction conditions with a yield of 90%, and the triazole analogs synthesized by click chemistry were suitable ligands for tricarbonyl rhenium.
Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai, People's Republic of China.
Cheng
C
Wang
Wei
W
Zhou
Junfeng
J
Yu
Lan
L
Zhang
Ni
N
Wang
D002851:Chromatography, High Pressure Liquid; D057930:Click Chemistry / Q000379:methods*; D006801:Humans; D007553:Isotope Labeling; D008024:Ligands; D009942:Organometallic Compounds / Q000138:chemical synthesis*; D011868:Radioisotopes / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D012211:Rhenium / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry
D008024:Ligands; D009942:Organometallic Compounds; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D014230:Triazoles; D012211:Rhenium