Facile and efficient synthesis of [18 F]Fluoromisonidazole using novel 2-nitroimidazole derivatives
[81F]Fluoromisonidazole ([ ([81F]FMISO) is a hypoxia imaging marker utilized in positron emission tomography. Novel FMISO precursors were prepared from a commercially available material, and several reaction factors that affect synthesis of [ [81F]FMISO were examined to achieve a higher fluorination yield. [18 F]FMISO was obtained from radiosynthesis, followed by the hydrolysis of protecting groups with HCl. New 2-nitroimidazole precursor showed a higher [18 F]fluorination and a higher synthetic yield. This result provided alternative guidelines for the preparation of hypoxia imaging marker.
Kwon, Young-Do,Jung, Yongju,Lim, B Seok Tae,Sohna, Myung-Hee,Kim, Hee-Kwon
p. 1150 - 1156
(2016/08/16)
Practical synthesis of 1-(2-Nitro-1H-imidazol-1-yl)-3-(tosyloxy) propan-2-yl acetate for the radiosynthesis of [18F]-FMISO
Hypoxia is related with many tumors due to a decreased oxygen condition. Novel synthesis for 1-(2-nitro-1H-imidazol-1-yl)-3-(tosyloxy)propan-2-yl acetate for the radiosynthesis of the [18F]-Flouromisonidazole ([18F]-FMISO), a hypoxia imaging marker used in positron emission tomography, from the readily available starting material is described. In this approach, one-pot two-step syntheses were used for the preparation of the [18F]-FMISO precursors that contain acetyl group. The mild reaction conditions and easy treatments are attractive features in this synthesis. This new synthetic route provides alternative choices for the preparation of hypoxia imaging marker.
A new and improved synthesis of the precursor of the hypoxia marker [ 18F]-FMISO
A new synthetic approach to the precursor of the hypoxia marker [ 18F]-FMISO has been developed. Three different tosylation methods were studied for the preparation of the key intermediate. The overall yield is markedly higher than the yields reported for previous syntheses. The precursor was used to prepare [18F]-FMISO and the results were comparable to those obtained when a commercial precursor was used.
Nieto, Elena,Alajarin, Ramon,Alvarez-Builla, Julio,Larranaga, Ignacio,Gorospe, Elena,Pozo, Miguel A.
experimental part
p. 3700 - 3704
(2010/12/25)
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